Name: Oridonin
Brand: Selleck Chemicals
SKU: S2335
Rating: 5 (25 reviews)

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Batch: Zuiverheid: 99.99%

99.99

Gerelateerde doelwitten	PI3K mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK
Overig Akt Inhibitoren	SC79 AZD5363 (Capivasertib) MK-2206 Dihydrochloride Ipatasertib (GDC-0068) Perifosine GSK690693 Triciribine (API-2) Afuresertib (GSK2110183) CCT128930 A-674563 HCl

Celkweek, behandeling & werkzame concentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	PMID
HL60	Cytotoxicity assay		48 hrs	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay, IC50=2.5μM	23819871
RAW264.7	Antiinflammatory assay		18 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 18 hrs by Griess method, IC50=5.2μM	23819871
K562	Antiproliferative assay		72 hrs	Antiproliferative activity against human K562 cells after 72 hrs by MTT assay, IC50=4.33μM	28165738
Bel7402	Antiproliferative assay		72 hrs	Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay, IC50=5.41μM	28165738
MGC803	Antiproliferative assay		72 hrs	Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay, IC50=9.06μM	28165738
KB/CP4	Antiproliferative assay		48 hrs	Antiproliferative activity against human KB/CP4 cells after 48 hrs by MTT assay, IC50=10.8μM	28165738
KB-3-1	Antiproliferative assay		48 hrs	Antiproliferative activity against human KB-3-1 cells after 48 hrs by MTT assay, IC50=13.24μM	28165738
BEL7404/CP20	Antiproliferative assay		48 hrs	Antiproliferative activity against human BEL7404/CP20 cells after 48 hrs by MTT assay, IC50=17.17μM	28165738
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50=17.89μM	28165738
Bel7404	Antiproliferative assay		48 hrs	Antiproliferative activity against human Bel7404 cells after 48 hrs by MTT assay, IC50=17.92μM	28165738
NCI-H460	Antiproliferative assay		48 hrs	Antiproliferative activity against human NCI-H460 cells after 48 hrs by MTT assay, IC50=20.51μM	28165738
NCI-H460/MX20	Antiproliferative assay		48 hrs	Antiproliferative activity against human NCI-H460/MX20 cells after 48 hrs by MTT assay, IC50=25.86μM	28165738
K562	Antiproliferative assay		72 hrs	Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=4.64μM	30921757
SGC7901	Antiproliferative assay		72 hrs	Antiproliferative activity against human SGC7901 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=7.13μM	30921757
Bel7402	Antiproliferative assay		72 hrs	Antiproliferative activity against human Bel7402 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=7.85μM	30921757
HL60	Antiproliferative assay		72 hrs	Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=9.46μM	30921757
PC3	Antiproliferative assay		72 hrs	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=10.07μM	30921757
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=18.15μM	30921757
L02	Cytotoxicity assay		72 hrs	Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=19.53μM	30921757
HCT116	Antiproliferative assay		48 hrs	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay, IC50=6.84μM	30981113
L02	Cytotoxicity assay		48 hrs	Cytotoxicity in human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay, IC50=6.97μM	30981113
Bel7402	Antiproliferative assay		48 hrs	Antiproliferative activity against human Bel7402 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay, IC50=9.59μM	30981113
MCF7	Antiproliferative assay		48 hrs	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay, IC50=17.56μM	30981113
MDA-MB-231	Antiproliferative assay		48 hrs	Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay, EC50=29.4μM	30981113
HCT116	Cell cycle arrest assay	3 uM	24 hrs	Induction in cell cycle arrest in human HCT116 cells assessed as inhibition in cyclin A protein expression level at 3 uM incubated for 24 hrs by Western blot analysis	30981113
HCT116	Cell cycle arrest assay	3 uM	24 hrs	Induction in cell cycle arrest in human HCT116 cells assessed as inhibition in cyclin B1 protein expression level at 3 uM incubated for 24 hrs by Western blot analysis	30981113
HCT116	Apoptotic assay	1 uM	24 hrs	Induction of apoptotic morphological change in human HCT116 cells assessed as loss of original morphology at 1 uM incubated for 24 hrs by haematoxylin-eosin staining based microscopic method	30981113
HCT116	Apoptotic assay	1 uM	24 hrs	Induction of apoptotic morphological change in human HCT116 cells assessed as formation of unstructured state at 1 uM incubated for 24 hrs by haematoxylin-eosin staining based microscopic method	30981113
HCT116	Apoptotic assay	1 uM	24 hrs	Induction of apoptotic morphological change in human HCT116 cells assessed as formation of volume swelling at 1 uM incubated for 24 hrs by haematoxylin-eosin staining based microscopic method	30981113
HCT116	Apoptotic assay	1 uM	24 hrs	Induction of apoptotic morphological change in human HCT116 cells assessed as formation of condensed nuclei at 1 uM incubated for 24 hrs by haematoxylin-eosin staining based microscopic method	30981113
HCT116	Apoptotic assay	1 uM	24 hrs	Induction of apoptotic morphological change in human HCT116 cells assessed as cell lysis at 1 uM incubated for 24 hrs by haematoxylin-eosin staining based microscopic method	30981113
HCT116	Apoptotic assay	1 uM	24 hrs	Induction of apoptotic morphological change in human HCT116 cells assessed as membrane shrinkage at 1 uM incubated for 24 hrs by haematoxylin-eosin staining based microscopic method	30981113
PLC/PRF/5	Antiproliferative assay		72 hrs	Antiproliferative activity against human PLC/PRF/5 cells incubated for 72 hrs by CCK8 cells, IC50=7.41μM	31200238
HepG2	Antiproliferative assay		72 hrs	Antiproliferative activity against human HepG2 cells incubated for 72 hrs by CCK8 cells, IC50=8.12μM	31200238
RPMI8226	Antiproliferative assay		72 hrs	Antiproliferative activity against human RPMI8226 cells incubated for 72 hrs by CCK8 cells, IC50=9.25μM	31200238
LO2	Cytotoxicity assay		72 hrs	Cytotoxicity against human LO2 cells incubated for 72 hrs by CCK8 cells, IC50=17.47μM	31200238
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells incubated for 72 hrs by CCK8 cells, IC50=30.4μM	31200238
HepG2	Function assay	0.1 to 1 uM	10 days	Inhibition of colony formation in human HepG2 cells at 0.1 to 1 uM incubated for 10 days by crystal violet staining based microscopic method	31200238
PLC/PRF/5	Function assay	0.001 to 1 uM	10 days	Inhibition of colony formation in human PLC/PRF/5 cells assessed as decrease in colony size at 0.001 to 1 uM incubated for 10 days by crystal violet staining based microscopic method	31200238
K562	Antiproliferative assay		72 hrs	Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=4.79μM	31202992
SGC7901	Antiproliferative assay		72 hrs	Antiproliferative activity against human SGC7901 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=7.87μM	31202992
Bel7402	Antiproliferative assay		72 hrs	Antiproliferative activity against human Bel7402 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=8.31μM	31202992
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=17.8μM	31202992
L02	Cytotoxicity assay		72 hrs	Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50=18.68μM	31202992
TE1	Antiproliferative assay		72 hrs	Antiproliferative activity against human TE1 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay, IC50=12.73μM	31494472
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay, IC50=13.45μM	31494472
MGC803	Antiproliferative assay		72 hrs	Antiproliferative activity against human MGC803 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay, IC50=14.13μM	31494472
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay, IC50=21.97μM	31494472
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit

Molecuulgewicht	364.43	Formule	C₂₀H₂₈O₆	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	28957-04-2	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel

Oplosbaarheid

In vitro
Batch:

DMSO : 72 mg/mL (197.56 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 34 mg/mL

Water : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Molecuulgewicht
=	×	×

Verdunningscalculator Molecuulgewichtcalculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	3.650mg/ml (10.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 73 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	0.600mg/ml (1.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo formulatiecalculator (heldere oplossing)

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

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

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

Targets/IC₅₀/Ki	Akt1 (Cell-free assay) 8.4 μM Akt2 (Cell-free assay) 8.9 μM
In vitro	Oridonin remt effectief de proliferatie van een breed scala aan kankercellen, waaronder die van prostaat (LNCaP, DU145, PC3), borst (MCF-7, MDA-MB231), niet-kleincellige longkanker (NSCL) (NCI-H520, NCI-H460, NCI-H1299), acute promyelocytische leukemie (NB4) en glioblastoma multiforme (U118, U138) met ED50's variërend van 1,8 tot 7,5 μg/ml. De antitumorale activiteiten van deze verbinding kunnen te wijten zijn aan de remmende effecten op de NF-kappaB- en MAPKs-signaalroutes.
In vivo	LD50: Muizen 35-40mg/kg.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/12964003/ [2] https://pubmed.ncbi.nlm.nih.gov/15827331/ [3] https://pubmed.ncbi.nlm.nih.gov/18094523/ [4] https://pubmed.ncbi.nlm.nih.gov/1269612/ [5] https://pubmed.ncbi.nlm.nih.gov/29695636/