Home Cytoskeletal Signaling Antineoplastic and Immunosuppressive Antibiotics Remmer Vincristine (Leurocristine) Sulfate

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Vincristine (Leurocristine) Sulfate Microtubuli-polymerisatieremmer

Cat.nr.S1241

Vincristinesulfaat is een remmer van de polymerisatie van microtubuli door binding aan tubuline met een IC50 van 32 μM in een celvrije test. Vincristinesulfaat induceert apoptose.
Vincristine (Leurocristine) Sulfate Antineoplastic and Immunosuppressive Antibiotics Remmer Chemical Structure

Chemische structuur

Molecuulgewicht: 923.04

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.94%
99.94

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen Assaytype Concentratie Incubatietijd Formulering Activiteitsbeschrijving PMID
HepG2.2.15 Cell Viability Assay 0-0.5 μM 24 h decreases cell viability dose dependently 25663769
HepG2-HBV1.1 Apoptosis Assay 0-0.5 μM 24 h induces apoptosis dose dependently 25663769
HepG2.2.15 Function Assay 0.1 μM 24 h promotes hepatitis B virus protein expression 25663769
HepG2-HBV1.1 Function Assay 0.1 μM 24 h promotes hepatitis B virus protein expression 25663769
HepG2-HBV1.1 Function Assay 0.1 μM 48 h promotes cell excretion of hepatitis B virus nucleocapsids instead of hepatitis B virus Dane particles 25663769
HepG2-HBV1.1 Growth Inhibition Assay 0.1 μM 1-5 d inhibits the proliferation time dependently 25663769
HepG2-HBV1.1 Growth Inhibition Assay 0.1 μM 1-5 d inhibits the proliferation time dependently 25663769
HepG2-HBV1.1 Growth Inhibition Assay 0.1 μM 12-72 h induces cell cycle arrest at S-phase 25663769
HepG2-HBV1.1 Growth Inhibition Assay 0.1 μM 12-72 h induces cell cycle arrest at S-phase 25663769
Raji Function Assay 0.5 μM 72 h abolishes autophagy  25446377
SK-MEL-28  Function Assay 30 nM 6 h induces G2–M cell-cycle arrest 25313010
H157 Growth Inhibition Assay IC50=1.03 ± 0.04 miu2M 25257911
Jurkat Growth Inhibition Assay 1-3 nM 48 h DMSO decreases viable cell numbers dose dependently 25156146
CEM Growth Inhibition Assay 1-3 nM 48 h DMSO decreases viable cell numbers dose dependently 25156146
P12 Growth Inhibition Assay 1-3 nM 48 h DMSO decreases viable cell numbers dose dependently 25156146
KB Growth Inhibition Assay IC50=0.0049 ± 0.0001 μM 25058526
KBv200 (ABCB1) Growth Inhibition Assay IC50=0.3462 ± 0.0066 μM 25058526
SUDHL6  Growth Inhibition Assay 1 μM 48/72 h inhibits cell viability significantly 24961604
SUDHL6  Function Assay 1 μM 72 h induces significant apoptotic morphology changes cotrested with BCL11A siRNA 24961604
HCT-116 Growth Inhibition Assay GI50=5 nM 24927857
SKNBe2C Growth Inhibition Assay IC50=32.8±4.0 nM 24921920
IGNR91 Growth Inhibition Assay IC50=24.3±1.7 nM 24921920
SKNAS Growth Inhibition Assay IC50=1.5±0.2 nM 24921920
LAN1 Growth Inhibition Assay IC50=2.3±0.2 nM 24921920
SHSY5Y Growth Inhibition Assay IC50=8.2±0.6 nM 24921920
A549-WT Growth Inhibition Assay IC50=19.437 ± 0.594 nM 24858827
A549-R Growth Inhibition Assay IC50=12.178 ± 0.333 nM 24858827
MCF-7-WT Growth Inhibition Assay IC50=17.752 ± 0.218 nM 24858827
MCF-7-R Growth Inhibition Assay IC50=5.539 ± 0.144 nM 24858827
A549-R Cytotoxicity Assay IC50=12.178 ± 0.333 nM 24858827
MCF-7-R Cytotoxicity Assay IC50=5.539 ± 0.144 nM 24858827
SW620 Growth Inhibition Assay IC50=7.80 ± 0.08 nM 24726739
SW620/AD300 Growth Inhibition Assay IC50=909.60 ± 8.91 nM 24726739
HEK293/pcDNA3.1 Growth Inhibition Assay IC50=1.45 ± 0.20 nM 24726739
HEK293/ABCC1 Growth Inhibition Assay IC50=19.29 ± 2.08 nM 24726739
TCC Growth Inhibition Assay 24 h IC50=70 nM 24716944
TCC Growth Inhibition Assay 48 h IC50=50 nM 24716944
HepG2/ADM Growth Inhibition Assay IC50=2.7863±0.2371 μM 24704556
HepG2 Growth Inhibition Assay IC50=0.0115±0.0017 μM 24704556
MCF-7/ADR Growth Inhibition Assay IC50=4.4826±0.2070 μM 24704556
MCF-7 Growth Inhibition Assay IC50=0.0159±0.0062 μM 24704556
A-172  Growth Inhibition Assay 0.1 μM 24/72 h inhibits cell growth time dependently 24530235
U-251MG Growth Inhibition Assay 0.1 μM 24/72 h inhibits cell growth time dependently 24530235
DLD-1 Function Assay 100 nM 48 h promotes RUNX3 demethylation  24403453
CCD18Co Function Assay 100 nM 48 h promotes RUNX3 demethylation  24403453
DLD-1 Growth Inhibition Assay 0-1000 nM 48 h inhibits cell growth dose dependently 24403453
CCD18Co Growth Inhibition Assay 0-1000 nM 48 h inhibits cell growth dose dependently 24403453
HepG2 Growth Inhibition Assay 24 h IC50=52.5 μM 24341688
HEK293/pcDNA3.1 Growth Inhibition Assay IC50=0.004±0.0003 μM 24284783
HEK293/MRP1 Growth Inhibition Assay IC50=0.055±0.0120 μM 24284783
Ramos Apoptosis Assay 2 μM 48 h induces 34.6%±1.92% apoptosis 24256491
NCI-H1299/pcDNA3 Cell Viability Assay 0-20 nM 96 h inhibits cell viability dose dependently 24177012
H1299/ICAM-3 Cell Viability Assay 0-20 nM 96 h inhibits cell viability dose dependently 24177012
NCI-H1299/pcDNA3 Function Assay 1/5/10/20 nM 96 h induces cleavage of caspases-3, 8, 9, and PARP 24177012
H1299/ICAM-3 Function Assay 1/5/10/20 nM 96 h induces cleavage of caspases-3, 8, 9, and PARP 24177012
W1 Growth Inhibition Assay IC50=0.0032 μM 24140176
W1VR Growth Inhibition Assay IC50=0.056 μM 24140176
K562 Growth Inhibition Assay IC50=0.032 ± 0.001 μM 24135937
K562/ADR Growth Inhibition Assay IC50=3.261 ± 0.412 μM 24135937
K562 Apoptosis Assay 0.3 μM 24 h induces apoptosis significantly 24135937
K562/ADR Apoptosis Assay 3 μM 24 h induces apoptosis 24135937
A549 Growth Inhibition Assay IC50=0.10 ± 0.03 μM 23971075
K562 Cell Viability Assay 3.75–60 nM 72 h  inhibits cell viability dose dependently 23877223
lucena Cell Viability Assay 3.75–60 nM 72 h  no effect 23877223
FEPS Cell Viability Assay 3.75–60 nM 72 h  no effect 23877223
A2780 Growth Inhibition Assay IC50=3.5 mM 23829203
ACHN Growth Inhibition Assay IC50<0.1 mM 23829203
U-937 Growth Inhibition Assay IC50<34 nM 23829203
Jurkat Apoptosis Assay 5 μg/ml  24 h induces apoptosis significantly 23810409
Jurkat Growth Inhibition Assay 5 μg/ml  24 h arrest Jurkat cells in G2/M phase 23810409
Hep-2 Growth Inhibition Assay IC50=0.04±0.01 μM 23780424
Hep-2/v Growth Inhibition Assay IC50=1.8±0.20 μM 23780424
SGC-7901 Growth Inhibition Assay 0-10 μg/ml 24/48/72 h inhibits cell growth in dose and time dependent manner 23743572
SGC-7901/VCR Growth Inhibition Assay 0-10 μg/ml 24/48/72 h inhibits cell growth in dose and time dependent manner 23743572
SGC-7901 Apoptosis Assay induces apoptosis significantly 23743572
SGC-7901/VCR Apoptosis Assay induces apoptosis significantly 23743572
KB-3-1 Growth Inhibition Assay IC50=1.66 ± 0.162 μM 23673445
KB-C2 Growth Inhibition Assay IC50=202.56 ± 42.481 μM 23673445
KB-3-1 Growth Inhibition Assay IC50=1.26 ± 0.027 μM 23673445
KB-V1 Growth Inhibition Assay IC50=208.85 ± 20.4 μM 23673445
HEK293/pcDNA3.1 Growth Inhibition Assay IC50=24.1 ± 0.204 μM 23673445
HEK293/ABCB1 Growth Inhibition Assay IC50=3512.8 ± 378.391 μM 23673445
A549/EGFP  Growth Inhibition Assay 0.01-1000 μM IC50=86.7 ± 29.1 μM 23634282
A549/Slug Growth Inhibition Assay 0.01-1000 μM IC50=9.7 ± 3.1 μM 23634282
JFCR39  Growth Inhibition Assay 1 µM 24 h DMSO markedly increases the number of G2/M phase cells 23598276
A549 Function Assay 100 nM 16 h DMSO leads to a loss of microtubules 23598276
SGC7901 Growth Inhibition Assay IC50=1.26 ± 0.11 μg/ml 23564482
SGC7901/LV-NC Growth Inhibition Assay IC50=1.77 ± 0.16 μg/ml 23564482
SGC7901/LV-SGO1 Growth Inhibition Assay IC50=4.36 ± 0.37 μg/ml 23564482
SGC7901/VCR Growth Inhibition Assay IC53=20.53 ± 1.96 μg/ml 23564482
SGC7901/VCR-NC Growth Inhibition Assay IC50=19.86 ± 2.01 μg/ml 23564482
SGC7901/VCR-si-SGO1 Growth Inhibition Assay IC50=6.18 ± 1.03 μg/ml 23564482
SGC7901/ADR Growth Inhibition Assay IC50=7.85 ± 0.64 μg/ml 23564482
SGC7901/ADR-NC Growth Inhibition Assay IC50=8.93 ± 0.68 μg/ml 23564482
SGC7901/ADR-si-SGO1 Growth Inhibition Assay IC50=3.46 ± 0.29 μg/ml 23564482
SH-SY5Y  Growth Inhibition Assay 0.001-10 μM 24 h IC50=0.113±0.012 μM 23129065
SH-SY5Y  Growth Inhibition Assay 0.001-10 μM 48 h IC50=0.078±0.009 μM 23129065
SH-SY5Y  Growth Inhibition Assay 0.001-10 μM 72 h IC50=0.051±0.008 μM 23129065
SH-SY5Y Apoptosis Assay 0.1 μM 0-24 h induces apoptosis of SH-SY5Y cells following cell cycle arrest at the G2/M phase 23129065
SH-SY5Y Apoptosis Assay 0.1 μM 0-24 h induces mitotic arrest  23129065
LNCAP Cytotoxicity assay 72 hrs Cytotoxicity against human LNCAP cells after 72 hrs by alamar blue assay, IC50 = 0.0029 μM. 20732809
LNCAP Cytotoxicity assay 72 hrs Cytotoxicity against human LNCAP cells after 72 hrs by alamar blue assay, IC50 = 0.0061 μM. 23215348
PC3 Cytotoxicity assay 72 hrs Cytotoxicity against human PC3 cells after 72 hrs by alamar blue assay, IC50 = 0.011 μM. 20732809
PC3 Cytotoxicity assay 72 hrs Cytotoxicity against human PC3 cells after 72 hrs by alamar blue assay, IC50 = 0.015 μM. 23215348
PC3 Cytotoxicity assay 72 hrs Cytotoxicity against human PC3 cells assessed as inhibition of cell viability after 72 hrs by alamar blue assay, IC50 = 0.0153 μM. 23489291
NFF Cytotoxicity assay 72 hrs Cytotoxicity against human NFF cells assessed as inhibition of cell viability after 72 hrs by alamar blue assay, IC50 = 0.0169 μM. 23489291
NFF Cytotoxicity assay 72 hrs Cytotoxicity against human NFF cells after 72 hrs by alamar blue assay, IC50 = 0.017 μM. 23215348
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by alamar blue assay, IC50 = 0.02 μM. 23215348
KB Cytotoxicity assay 72 hrs Cytotoxicity against human KB cells after 72 hrs by SRB assay, IC50 = 0.02 μM. 26522953
PC3 Antiproliferative assay 48 hrs Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay, IC50 = 0.0276 μM. 28038323
HEK Cytotoxicity assay 72 hrs Cytotoxicity against human HEK cells after 72 hrs by alamar blue assay, IC50 = 0.031 μM. 23215348
HeLa Cytotoxicity assay 72 hrs Cytotoxicity against human HeLa cells assessed as inhibition of cell viability after 72 hrs by alamar blue assay, IC50 = 0.0358 μM. 23489291
HeLa Cytotoxicity assay 72 hrs Cytotoxicity against human HeLa cells after 72 hrs by alamar blue assay, IC50 = 0.036 μM. 23215348
BT549 Antiproliferative assay 48 hrs Antiproliferative activity against human BT549 cells after 48 hrs by MTT assay, IC50 = 0.05472 μM. 28038323
DU145 Antiproliferative assay 48 hrs Antiproliferative activity against human DU145 cells after 48 hrs by MTT assay, IC50 = 0.0723 μM. 28038323
Leukemia cells Antitumor assay 48 hrs Antitumor activity against human Leukemia cells after 48 hrs by SRB assay, GI50 = 0.1 μM. 19006285
Leukemia cells Antitumor assay 48 hrs Antitumor activity against human Leukemia cells after 48 hrs by SRB assay, GI = 0.1 μM. 19006285
Colon cancer cells Cytotoxicity assay Cytotoxicity against human colon cancer cells, GI50 = 0.1 μM. 18598018
Leukemia cells Cytotoxicity assay Cytotoxicity against human leukemia cells, GI50 = 0.1 μM. 18598018
Colon cancer cells Antitumor assay 48 hrs Antitumor activity against human Colon cancer cells after 48 hrs by SRB assay, GI50 = 0.1 μM. 19006285
Colon cancer cells Antitumor assay 48 hrs Antitumor activity against human Colon cancer cells after 48 hrs by SRB assay, GI = 0.1 μM. 19006285
Leukemia cells Antitumor assay Antitumor activity against leukemia cells, GI50 = 0.1 μM. 17559205
Colon cancer cells Antitumor assay Antitumor activity against colon tumor cells, GI50 = 0.1 μM. 17559205
Leukemia cells Growth inhibition assay 48 hrs Growth inhibition of human leukemia cells after 48 hrs, GI50 = 0.1 μM. 20684599
Colon cancer cells Growth inhibition assay 48 hrs Growth inhibition of human colon cancer cells after 48 hrs, GI50 = 0.1 μM. 20684599
Leukemia cells Cytotoxicity assay 48 hrs Cytotoxicity against human leukemia cells after 48 hrs, GI50 = 0.1 μM. 24747749
Colon cancer cells Cytotoxicity assay 48 hrs Cytotoxicity against human colon cancer cells after 48 hrs, GI50 = 0.1 μM. 24747749
Leukemia cells Cytotoxicity assay 48 hrs Cytotoxicity against human leukemia cells after 48 hrs, GI50 = 0.1 μM. 22283430
Colon cancer cells Cytotoxicity assay 48 hrs Cytotoxicity against human COLON cells after 48 hrs, GI50 = 0.1 μM. 22283430
MDA-MB-231 Antiproliferative assay 48 hrs Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50 = 0.1166 μM. 28038323
central nervous system cancer cells Cytotoxicity assay Cytotoxicity against human central nervous system cancer cells, GI50 = 0.12589 μM. 18598018
prostate cancer cells Cytotoxicity assay Cytotoxicity against human prostate cancer cells, GI50 = 0.12589 μM. 18598018
CNS Antitumor assay 48 hrs Antitumor activity against human CNS cancer cells after 48 hrs by SRB assay, GI50 = 0.12589 μM. 19006285
prostate cancer cells Antitumor assay 48 hrs Antitumor activity against human prostate cancer cells after 48 hrs by SRB assay, GI50 = 0.12589 μM. 19006285
CNS Antitumor assay Antitumor activity against CNS tumor cells, GI50 = 0.12589 μM. 17559205
prostate cancer cells Antitumor assay Antitumor activity against prostate tumor cells, GI50 = 0.12589 μM. 17559205
CNS Antitumor assay 48 hrs Antitumor activity against human CNS cancer cells after 48 hrs by SRB assay, GI = 0.13 μM. 19006285
prostate cancer cells Antitumor assay 48 hrs Antitumor activity against human prostate cancer cells after 48 hrs by SRB assay, GI = 0.13 μM. 19006285
prostate cancer cells Growth inhibition assay 48 hrs Growth inhibition of human prostate cancer cells after 48 hrs, GI50 = 0.13 μM. 20684599
CNS Growth inhibition assay 48 hrs Growth inhibition of human CNS cancer cells after 48 hrs, GI50 = 0.13 μM. 20684599
CNS Cytotoxicity assay 48 hrs Cytotoxicity against human CNS cancer cells after 48 hrs, GI50 = 0.13 μM. 24747749
prostate cancer cells Cytotoxicity assay 48 hrs Cytotoxicity against human prostate cancer cells after 48 hrs, GI50 = 0.13 μM. 24747749
prostate cancer cells Cytotoxicity assay 48 hrs Cytotoxicity against human prostate cancer cells after 48 hrs, GI50 = 0.13 μM. 22283430
CNS Cytotoxicity assay 48 hrs Cytotoxicity against human CNS cancer cells after 48 hrs, GI50 = 0.13 μM. 22283430
Melanoma cells Antitumor assay 48 hrs Antitumor activity against human Melanoma cells after 48 hrs by SRB assay, GI50 = 0.15849 μM. 19006285
Melanoma cells Cytotoxicity assay Cytotoxicity against human melanoma cells, GI50 = 0.15849 μM. 18598018
Melanoma cells Antitumor assay Antitumor activity against melanoma cells, GI50 = 0.15849 μM. 17559205
Melanoma cells Antitumor assay 48 hrs Antitumor activity against human Melanoma cells after 48 hrs by SRB assay, GI = 0.16 μM. 19006285
Melanoma cells Growth inhibition assay Growth inhibition of human melanoma cells after 48 hrs, GI50 = 0.16 μM. 20684599
Melanoma cells Cytotoxicity assay 48 hrs Cytotoxicity against human melanoma cells after 48 hrs, GI50 = 0.16 μM. 24747749
Melanoma cells Cytotoxicity assay 48 hrs Cytotoxicity against human melanoma cells after 48 hrs, GI50 = 0.16 μM. 22283430
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 0.1715 μM. 28038323
NSCLC Antitumor assay 48 hrs Antitumor activity against human NSCLC cells after 48 hrs by SRB assay, GI = 0.25 μM. 19006285
NSCLC Growth inhibition assay 48 hrs Growth inhibition of human NSCLC cells after 48 hrs, GI50 = 0.25 μM. 20684599
NSCLC Cytotoxicity assay 48 hrs Cytotoxicity against human NSCLC cells after 48 hrs, GI50 = 0.25 μM. 22283430
NSCLC Cytotoxicity assay 48 hrs Cytotoxicity against human NSCLC cells after 48 hrs, GI50 = 0.25 μM. 24747749
NSCLC Antitumor assay Antitumor activity against NSCLC cells, GI50 = 0.25119 μM. 17559205
NSCLC Antitumor assay 48 hrs Antitumor activity against human NSCLC cells after 48 hrs by SRB assay, GI50 = 0.25119 μM. 19006285
Non-small cell lung carcinoma cells Cytotoxicity assay Cytotoxicity against human Non-small cell lung carcinoma cells, GI50 = 0.25119 μM. 18598018
ovarian cancer cells Cytotoxicity assay Cytotoxicity against human ovarian cancer cells, GI50 = 0.31623 μM. 18598018
renal cancer cells Cytotoxicity assay Cytotoxicity against human renal cancer cells, GI50 = 0.31623 μM. 18598018
breast cancer cells Cytotoxicity assay Cytotoxicity against human breast cancer cells, GI50 = 0.31623 μM. 18598018
ovarian cancer cells Antitumor assay 48 hrs Antitumor activity against human ovarian cancer cells after 48 hrs by SRB assay, GI50 = 0.31623 μM. 19006285
renal cancer cells Antitumor assay 48 hrs Antitumor activity against human renal cancer cells after 48 hrs by SRB assay, GI50 = 0.31623 μM. 19006285
breast cancer cells Antitumor assay 48 hrs Antitumor activity against human Breast cancer cells after 48 hrs by SRB assay, GI50 = 0.31623 μM. 19006285
renal cancer cells Antitumor assay Antitumor activity against renal tumor cells, GI50 = 0.31623 μM. 17559205
ovarian cancer cells Antitumor assay Antitumor activity against ovarian tumor cells, GI50 = 0.31623 μM. 17559205
breast cancer cells Antitumor assay Antitumor activity against breast tumor cells, GI50 = 0.31623 μM. 17559205
ovarian cancer cells Antitumor assay 48 hrs Antitumor activity against human ovarian cancer cells after 48 hrs by SRB assay, GI = 0.32 μM. 19006285
renal cancer cells Antitumor assay 48 hrs Antitumor activity against human renal cancer cells after 48 hrs by SRB assay, GI = 0.32 μM. 19006285
breast cancer cells Antitumor assay 48 hrs Antitumor activity against human Breast cancer cells after 48 hrs by SRB assay, GI = 0.32 μM. 19006285
renal cancer cells Growth inhibition assay 48 hrs Growth inhibition of human renal cancer cells after 48 hrs, GI50 = 0.32 μM. 20684599
breast cancer cells Growth inhibition assay 48 hrs Growth inhibition of human breast cancer cells after 48 hrs, GI50 = 0.32 μM. 20684599
ovarian cancer cells Growth inhibition assay 48 hrs Growth inhibition of human Ovarian cancer cells after 48 hrs, GI50 = 0.32 μM. 20684599
breast cancer cells Cytotoxicity assay 48 hrs Cytotoxicity against human breast cancer cells after 48 hrs, GI50 = 0.32 μM. 24747749
renal cancer cells Cytotoxicity assay 48 hrs Cytotoxicity against human renal cancer cells after 48 hrs, GI50 = 0.32 μM. 24747749
ovarian cancer cells Cytotoxicity assay 48 hrs Cytotoxicity against human ovarian cancer cells after 48 hrs, GI50 = 0.32 μM. 24747749
renal cancer cells Cytotoxicity assay 48 hrs Cytotoxicity against human renal cancer cells after 48 hrs, GI50 = 0.32 μM. 22283430
ovarian cancer cells Cytotoxicity assay 48 hrs Cytotoxicity against human ovarian cancer cells after 48 hrs, GI50 = 0.32 μM. 22283430
breast cancer cells Cytotoxicity assay 48 hrs Cytotoxicity against human breast cancer cells after 48 hrs, GI50 = 0.32 μM. 22283430
Lu1 Cytotoxicity assay 72 hrs Cytotoxicity against human Lu1 cells after 72 hrs by SRB assay, IC50 = 0.48 μM. 26522953
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay, IC50 = 0.51 μM. 26522953
HepG2 Cytotoxicity assay 72 hrs Cytotoxicity against human HepG2 cells after 72 hrs by SRB assay, IC50 = 0.69 μM. 26522953
COLON Growth inhibition assay 48 hrs Growth inhibition of human colon cancer cells after 48 hrs, TGI = 3.98 μM. 20684599
COLON Cytotoxicity assay 48 hrs Cytotoxicity against human colon cancer cells after 48 hrs, TGI = 3.98 μM. 24747749
COLON Cytotoxicity assay 48 hrs Cytotoxicity against human COLON cells after 48 hrs, TGI = 3.98 μM. 22283430
COLON Cytotoxicity assay Cytotoxicity against human colon cancer cells, TGI = 3.98107 μM. 18598018
COLON Antitumor assay 48 hrs Antitumor activity against human Colon cancer cells after 48 hrs by SRB assay, TGI = 3.98107 μM. 19006285
COLON Antitumor assay Antitumor activity against colon tumor cells, TGI = 3.98107 μM. 17559205
central nervous system cancer cells Cytotoxicity assay Cytotoxicity against human central nervous system cancer cells, TGI = 6.30957 μM. 18598018
prostate cancer cells Cytotoxicity assay Cytotoxicity against human prostate cancer cells, TGI = 6.30957 μM. 18598018
CNS Antitumor assay 48 hrs Antitumor activity against human CNS cancer cells after 48 hrs by SRB assay, TGI = 6.30957 μM. 19006285
prostate cancer cells Antitumor assay 48 hrs Antitumor activity against human prostate cancer cells after 48 hrs by SRB assay, TGI = 6.30957 μM. 19006285
CNS Antitumor assay Antitumor activity against CNS tumor cells, TGI = 6.30957 μM. 17559205
prostate cancer cells Antitumor assay Antitumor activity against prostate tumor cells, TGI = 6.30957 μM. 17559205
prostate cancer cells Growth inhibition assay 48 hrs Growth inhibition of human prostate cancer cells after 48 hrs, TGI = 6.31 μM. 20684599
CNS Growth inhibition assay 48 hrs Growth inhibition of human CNS cancer cells after 48 hrs, TGI = 6.31 μM. 20684599
CNS Cytotoxicity assay 48 hrs Cytotoxicity against human CNS cancer cells after 48 hrs, TGI = 6.31 μM. 24747749
prostate cancer cells Cytotoxicity assay 48 hrs Cytotoxicity against human prostate cancer cells after 48 hrs, TGI = 6.31 μM. 24747749
prostate cancer cells Cytotoxicity assay 48 hrs Cytotoxicity against human prostate cancer cells after 48 hrs, TGI = 6.31 μM. 22283430
CNS Cytotoxicity assay 48 hrs Cytotoxicity against human CNS cancer cells after 48 hrs, TGI = 6.31 μM. 22283430
Melanoma cells Growth inhibition assay 48 hrs Growth inhibition of human melanoma cells after 48 hrs, TGI = 7.94 μM. 20684599
breast cancer cells Growth inhibition assay 48 hrs Growth inhibition of human breast cancer cells after 48 hrs, TGI = 7.94 μM. 20684599
breast cancer cells Cytotoxicity assay 48 hrs Cytotoxicity against human breast cancer cells after 48 hrs, TGI = 7.94 μM. 24747749
Melanoma cells Cytotoxicity assay 48 hrs Cytotoxicity against human melanoma cells after 48 hrs, TGI = 7.94 μM. 24747749
Melanoma cells Cytotoxicity assay 48 hrs Cytotoxicity against human melanoma cells after 48 hrs, TGI = 7.94 μM. 22283430
breast cancer cells Cytotoxicity assay 48 hrs Cytotoxicity against human breast cancer cells after 48 hrs, TGI = 7.94 μM. 22283430
Melanoma cells Antitumor assay 48 hrs Antitumor activity against human Melanoma cells after 48 hrs by SRB assay, TGI = 7.94328 μM. 19006285
Melanoma cells Cytotoxicity assay Cytotoxicity against human melanoma cells, TGI = 7.94328 μM. 18598018
breast cancer cells Cytotoxicity assay Cytotoxicity against human breast cancer cells, TGI = 7.94328 μM. 18598018
breast cancer cells Antitumor assay 48 hrs Antitumor activity against human Breast cancer cells after 48 hrs by SRB assay, TGI = 7.94328 μM. 19006285
Melanoma cells Antitumor assay Antitumor activity against melanoma cells, TGI = 7.94328 μM. 17559205
breast tumor cells Antitumor assay Antitumor activity against breast tumor cells, TGI = 7.94328 μM. 17559205
NSCLC Antitumor assay Antitumor activity against NSCLC cells, TGI = 15.8489 μM. 17559205
Leukemia cells Antitumor assay 48 hrs Antitumor activity against human Leukemia cells after 48 hrs by SRB assay, TGI = 15.8489 μM. 19006285
NSCLC Antitumor assay 48 hrs Antitumor activity against human NSCLC cells after 48 hrs by SRB assay, TGI = 15.8489 μM. 19006285
Non-small cell lung carcinoma cells Cytotoxicity assay Cytotoxicity against human Non-small cell lung carcinoma cells, TGI = 15.8489 μM. 18598018
Leukemia cells Cytotoxicity assay Cytotoxicity against human leukemia cells, TGI = 15.8489 μM. 18598018
Leukemia cells Antitumor assay Antitumor activity against leukemia cells, TGI = 15.8489 μM. 17559205
NSCLC Growth inhibition assay 48 hrs Growth inhibition of human NSCLC cells after 48 hrs, TGI = 15.85 μM. 20684599
Leukemia cells Growth inhibition assay 48 hrs Growth inhibition of human leukemia cells after 48 hrs, TGI = 15.85 μM. 20684599
NSCLC Cytotoxicity assay 48 hrs Cytotoxicity against human NSCLC cells after 48 hrs, TGI = 15.85 μM. 22283430
Leukemia cells Cytotoxicity assay 48 hrs Cytotoxicity against human leukemia cells after 48 hrs, TGI = 15.85 μM. 24747749
NSCLC Cytotoxicity assay 48 hrs Cytotoxicity against human NSCLC cells after 48 hrs, TGI = 15.85 μM. 24747749
Leukemia cells Cytotoxicity assay 48 hrs Cytotoxicity against human leukemia cells after 48 hrs, TGI = 15.85 μM. 22283430
renal cancer cells Growth inhibition assay 48 hrs Growth inhibition of human renal cancer cells after 48 hrs, TGI = 19.95 μM. 20684599
ovarian cancer cells Growth inhibition assay 48 hrs Growth inhibition of human Ovarian cancer cells after 48 hrs, TGI = 19.95 μM. 20684599
renal cancer cells Cytotoxicity assay 48 hrs Cytotoxicity against human renal cancer cells after 48 hrs, TGI = 19.95 μM. 24747749
ovarian cancer cells Cytotoxicity assay 48 hrs Cytotoxicity against human ovarian cancer cells after 48 hrs, TGI = 19.95 μM. 24747749
renal cancer cells Cytotoxicity assay 48 hrs Cytotoxicity against human renal cancer cells after 48 hrs, TGI = 19.95 μM. 22283430
ovarian cancer cells Cytotoxicity assay 48 hrs Cytotoxicity against human ovarian cancer cells after 48 hrs, TGI = 19.95 μM. 22283430
ovarian cancer cells Cytotoxicity assay Cytotoxicity against human ovarian cancer cells, TGI = 19.9526 μM. 18598018
renal cancer cells Cytotoxicity assay Cytotoxicity against human renal cancer cells, TGI = 19.9526 μM. 18598018
ovarian cancer cells Antitumor assay 48 hrs Antitumor activity against human ovarian cancer cells after 48 hrs by SRB assay, TGI = 19.9526 μM. 19006285
renal cancer cells Antitumor assay 48 hrs Antitumor activity against human renal cancer cells after 48 hrs by SRB assay, TGI = 19.9526 μM. 19006285
renal tumor cells Antitumor assay Antitumor activity against renal tumor cells, TGI = 19.9526 μM. 17559205
ovarian tumor cells Antitumor assay Antitumor activity against ovarian tumor cells, TGI = 19.9526 μM. 17559205
PC3 Cytotoxicity assay 48 hrs Cytotoxicity against human PC3 cells assessed as inhibition of cell viability after 48 hrs by MTT assay, IC50 = 28.11 μM. 29174816
neural precursor cells Function assay Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay 17417631
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Molecuulgewicht 923.04 Formule

C46H58N4O14S

 Opslag (vanaf de datum van ontvangst)
CAS-nr. 2068-78-2 SDF downloaden Opslag van stamoplossingen

Synoniemen Leurocristine sulfate, NSC-67574 sulfate, 22-Oxovincaleukoblastine sulfate Smiles CCC1(CC2CC(C3=C(CCN(C2)C1)C4=CC=CC=C4N3)(C5=C(C=C6C(=C5)C78CCN9C7C(C=CC9)(C(C(C8N6C=O)(C(=O)OC)O)OC(=O)C)CC)OC)C(=O)OC)O.OS(=O)(=O)O

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 100 mg/mL (108.33 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : 100 mg/mL

Ethanol : Insoluble

Molariteitscalculator

Massa Concentratie Volume Molecuulgewicht
Verdunningscalculator Molecuulgewichtcalculator

In vivo
Batch:

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

mg/kg g μL

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH2O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (Mechanism of Action)

Targets/IC50/Ki
Microtubules
(Cell-free assay)
32 μM
In vitro
Vincristinesulfaat remt de netto toevoeging van tubulinedimeren aan de assemblage-uiteinden van stabiele microtubuli met een Ki van 85 nM. Bij lage concentraties stabiliseert deze verbinding het spoelapparaat, wat resulteert in het falen van de chromosomen om te segregeren, leidend tot metafase-arrest en remming van mitose. Bij hogere concentraties kan het microtubuli verstoren en volledige depolymerisatie induceren. Deze chemische stof induceert apoptose in tumorcellen en remt de proliferatie van SH-SY5Y-cellen met een IC50 van 0,1 μM. Het induceert mitotische arrestatie en bevordert de expressie van caspase-3 en -9 en cycline B, terwijl de expressie van cycline D afneemt. De geïnduceerde neurotoxiciteit wordt veroorzaakt door interferentie met de microtubulifunctie, wat resulteert in blokkering van axonaal transport en daardoor in axonale degeneratie.
In vivo
Vincristinesulfaat (3 mg/kg) toegediend via een enkele i.p.-injectie aan muizen met bilaterale subcutane xenografts Rh12 of Rh18, induceert een gemiddelde groeivertraging van >120 en >52 dagen, en repopulatiefracties van respectievelijk 0,06% en 5%. Deze verbinding werkt op subcutane colon 38-tumoren bij muizen door gastheercelgemedieerde vasculaire effecten, evenals door directe tubuline-gemedieerde cytotoxiciteit. Het (5 mg/kg) vermindert de bloedstroom van tumoren met bijna 75%.
Referenties
  • [4] https://pubmed.ncbi.nlm.nih.gov/558047/
  • [5] https://pubmed.ncbi.nlm.nih.gov/3190743/
  • [6] https://pubmed.ncbi.nlm.nih.gov/1827725/

Toepassingen (Applications)

Methoden Biomarkers Afbeeldingen PMID
Western blot MPM2 / Cyclin B1 / Cdc25c / p-Cdc2 / Cdc2 / Aurora B / p-H3 / p-PLK1
S1241-WB1
26156322
Growth inhibition assay Cell viability
S1241-viability1
26156322

Informatie over klinische proeven (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer Werving Aandoeningen Sponsor/medewerkers Startdatum Fasen
NCT05844670 Recruiting
Pediatric Cancer
Moi University|Princess Maxima Center for Pediatric Oncology|Amsterdam UMC location VUmc
 April 20 2023 Phase 4
NCT04448834 Withdrawn
B-cell Acute Lymphoblastic Leukemia
Dorothy Sipkins MD PhD|Amgen|Acrotech Biopharma Inc.|Duke University
 January 2022 Phase 2

Veelgestelde vragen (Frequently Asked Questions)

Vraag 1:
I want to use it for mouse in vivo, could you please give us your advice about administration method?

Antwoord:
According to the reference cited on our website, we test its solubility in 4% DMSO/saline, and it is a suspension at 5 mg/mL. This compound can also be dissolved in the vehicle 4% DMSO/30% PEG 300/10% Tween 80/saline at 5 mg/ml as a clear solution for injection.