Name: Cyclophosphamide Monohydrate
Brand: Selleck Chemicals
SKU: S2057
Rating: 5 (40 reviews)

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.20%

99.20

Gerelateerde doelwitten	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase
Overig Alkylating Agent Inhibitoren	Berberine (Umbellatine) MNNG (1-Methyl-3-nitro-1-nitrosoguanidine)

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

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	PMID
HL60 cells	Cytotoxicity assay			Cytotoxicity against human HL60 cells by MTT assay, IC50=8.79 μM	20850303
BALB/c 3T3 cells	Cytotoxicity assay			In vitro cytotoxicity was evaluated in mouse embryo BALB/c 3T3 cells, IC50=37.6 μM	9873412
BALB/c 3T3	Cytotoxicity assay			In vitro cytotoxicity against BALB/c 3T3 cells, IC50 = 37.6 μM.	7877150
T-cells	Immunosuppressive assay	100 mg/kg	8 days	Immunosuppressive activity against MAV-1 infected BALB/c mouse assessed as T cells suppression at 100 mg/kg, ip treated 8 days before infection for 4 weeks measured 14 days post infection by flow cytometry	18268085
B-cells	Immunosuppressive assay	100 mg/kg	8 days	Immunosuppressive activity against MAV-1 infected BALB/c mouse assessed as B cells suppression at 100 mg/kg, ip treated 8 days before infection for 4 weeks measured 14 days post infection by flow cytometry	18268085
U87 MG	Antitumor assay	80 mg/kg		Antitumor activity in human U87 MG cells xenografted mouse at 80 mg/kg, iv administered in Q2D x 5 schedule	18450456
MX1	Antitumor assay	120 mg/kg	up to 3 weeks	Antitumor activity against human MX1 cells xenografted in nude mouse adjuvant model assessed as increase in mouse survival time at 120 mg/kg, po BID measured up to 3 weeks	20726512
U87MG	Anticancer assay	80 mg/kg	6 days	Anticancer activity against human U87MG cells xenografted in athymic mouse assessed as tumor suppression at 80 mg/kg, iv Q2D for 6 days	21106377
NCI-H522	Antitumor assay	50 mg/kg	28 days	Antitumor activity against human NCI-H522 cells xenografted in Balb/c nude mouse assessed as tumor growth inhibition at 50 mg/kg, ig administered once daily for 28 days relative to control	28092860
U2932	Antitumor assay	50 mg/kg	5 consecutive days	Antitumor activity against human U2932 cells xenografted in SCID mouse assessed as reduction in tumor burden at 50 mg/kg, ip administered for 5 consecutive days measured up to day 40 post cell injection	28605593
MDA-MB-231	Cytotoxicity assay		48 hr	Cytotoxicity against Homo sapiens (human) MDA-MB-231 cells after 48 hr by MTT assay, IC50 = 0.09 μM.	ChEMBL
K562	Cytotoxicity assay		48 hr	Cytotoxicity against Homo sapiens (human) K562 cells after 48 hr by MTT assay, IC50 = 0.15 μM.	ChEMBL
K562	Antiproliferative assay		48 hr	Antiproliferative activity against Homo sapiens (human) K562 cells after 48 hr by MTT assay, IC50 = 0.153 μM.	ChEMBL
MCF7	Cytotoxicity assay		48 hr	Cytotoxicity against Homo sapiens (human) MCF7 cells after 48 hr by SRB assay, IC50 = 10 mM.	19372630
HepG2	Cytotoxicity assay		48 hr	Cytotoxicity against Homo sapiens (human) HepG2 cells after 48 hr by MTT assay, IC50 = 0.24 μM.	ChEMBL
Klik om meer experimentele gegevens over cellijnen te bekijken

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

Molecuulgewicht	279.1	Formule	C₇H₁₅Cl₂N₂O₂P.H₂O	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	6055-19-2	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	NSC-26271 Monohydrate			Smiles	C1CNP(=O)(OC1)N(CCCl)CCCl.O

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 55 mg/mL (197.06 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : 55 mg/mL

Ethanol : 55 mg/mL

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.
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.	2.800mg/ml (10.03mM)	Taking the 1 mL working solution as an example, add 50 μL of clarified DMSO stock solution of 56 mg/ml to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; 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.
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.

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 (Mechanism of Action)

In vitro	Cyclophosphamide (CY) is a chemotherapeutic agent with a dose-dependent, bimodal effect on the immune system. Cyclophosphamide treatment enhances apoptosis and decreases homeostatic proliferation of regulatory T cells. Cyclophosphamide downregulates the expression of GITR and FoxP3, which are involved in the suppressive activity of T(REGs). Cyclophosphamide increases CYP3A4, CYP2C8, and CYP2C9 protein levels in primary human hepatocyte cultures, which thereby enhances their own rates of 4-hydroxylation in the cultured hepatocytes. Cyclophosphamide has produced mutations in base-pair substituting strains of Salmonella tryphimurium in the presence of metabolic activation, but it has been shown to be negative in the E. coli chromotest. Cyclophosphamide has been shown to produce gene mutations, chromosome aberrations, micronuclei and sister chromatid exchanges in a variety of cultured cells in the presence of metabolic activation as well as sister chromatid exchanges without metabolic activation.
In vivo	Cyclophosphamide has also produced chromosome damage and micronuclei in rats, mice and Chinese hamsters, and gene mutations in the mouse spot test and in the transgenic lacZ construct of Muta Mouse. Cyclophosphamide, when given in a defined sequence with a GM-CSF-secreting, neu-expressing whole-cell vaccine, enhances the vaccine's potential to delay tumor growth in neu transgenic mice. Cyclophosphamide mediates its effects by enhancing the efficacy of the vaccine rather than via a direct cytolytic effect on cancer cells.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/15591121/ [2] https://pubmed.ncbi.nlm.nih.gov/9157990/ [3] https://pubmed.ncbi.nlm.nih.gov/7623863/ [4] https://pubmed.ncbi.nlm.nih.gov/11325840/ [5] https://pubmed.ncbi.nlm.nih.gov/35409194/ [6] https://pubmed.ncbi.nlm.nih.gov/34385713/ [7] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7123643/ [8] https://pubmed.ncbi.nlm.nih.gov/21530682/

Toepassingen (Applications)

Methoden	Biomarkers	PMID
Western blot	PTEN / pAkt / Caspase 3 / GAPDH Caspase 3 / Cleaved-Caspase 3 / Cleaved-PARP / Tubulin Nuclear AIF / Cytosolic AIF / TBP / GAPDH LC3B I / LC3B II / GAPDH	23874108
Growth inhibition assay	Cell Viability Tumor Volume Tumor Volume	31429028
IHC	tumor cell invasion TUNEL / Caspase 3 PTEN / pAkt / PCNA ovary of mice Caspase-3	23874108
Immunofluorescence	pAKT / pERK Ki-67 / UPK3 / KRT5 / pERK Ki-67 / KRT14 / KRT5 autophagy levels	31654636

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
NCT06186700	Active not recruiting	Breast Cancer Female	Mansoura University	December 25 2023	Phase 2
NCT06085742	Recruiting	Breast Cancer	University of Illinois at Chicago	November 22 2023	Phase 2
NCT05800041	Not yet recruiting	Gout Tophus	RenJi Hospital\|Westlake Therapeutics	April 10 2023	Early Phase 1

Veelgestelde vragen (Frequently Asked Questions)

Vraag 1:
Why does it show no activity in vitro assays?

Antwoord:
The activity of this compound in vitro is controversial and has not been fully determined. It is a prodrug and may need Cytochrome P450 to convert it to the active form: 4-hydroxy cyclophosphamide. It is widely used in vivo, if you are going to use it in vitro, you may need to supplement Cytochrome P450 exogenously.

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Cyclophosphamide Monohydrate Alkylating Agent

Molecuulgewicht: 279.1

Kwaliteitscontrole (Quality Control)

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

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

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo formulatiecalculator (heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Toepassingen (Applications)

Informatie over klinische proeven (Clinical Trial Information)

Veelgestelde vragen (Frequently Asked Questions)

Cyclophosphamide Monohydrate Alkylating Agent

Molecuulgewicht: 279.1

Kwaliteitscontrole (Quality Control)

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

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

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo formulatiecalculator (heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Toepassingen (Applications)

Informatie over klinische proeven (Clinical Trial Information)

Veelgestelde vragen (Frequently Asked Questions)

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