research use only
Cat.No.S1217
| Related Targets | HDAC PARP ATM/ATR DNA-PK WRN Topoisomerase PPAR Sirtuin Casein Kinase eIF |
|---|---|
| Other DNA/RNA Synthesis Inhibitors | CX-5461 (Pidnarulex) B02 SCR7 Favipiravir (T-705) EED226 RK-33 BMH-21 Triapine (3-AP) Carmofur YK-4-279 |
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In vitro |
DMSO
: 52 mg/mL
(199.16 mM)
Water : 52 mg/mL Ethanol : 52 mg/mL |
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In vivo |
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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.
| Molecular Weight | 261.09 | Formula | C7H15Cl2N2O2P |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 50-18-0 | Download SDF | Storage of Stock Solutions |
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| Synonyms | NSC 26271,Endoxan, Cytoxan, Neosar, Procytox, Revimmune, Cytophosphane | Smiles | ClCCN(CCCl)[P]1(=O)NCCCO1 | ||
| Targets/IC50/Ki |
DNA replication
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|---|---|
| In vivo |
Cyclophosphamide is an alkylating agent with cytotoxic and immunosuppressive activities. This compound requires enzymatic and chemical activation to release active phosphoramide mustard which produces the interstrand and intrastrand DNA crosslinks at guanine N-7 positions. It exerts its cytotoxic activity by inhibiting nuclear DNA replication. The mechanism of this compound-induced immunosuppression is possibly due to direct cytotoxic effect of the drug on immunocompetent lymphocytes, particulafly those that have undergone antigenic differentiation and division. This chemical has its greatest effect on B cells with relative T cell-sparing effect. Trials in various tumor-bearing animals confirmed this in vivo activity and demonstrated fairly potent antitumor effect. This agent, in combination with other antineoplastic agents, is used for the treatment of various cancers, including breast, lymphoid and pediatric malignancies. |
References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| 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 |
Tel: +1-832-582-8158 Ext:3
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Question 1:
Why does it show no activity in in vitro assays in S1217?
Answer:
The activity of this product 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. This compound is widely used in vivo, if you are going to use it in vitro, you may need to supplement Cytochrome P450 exogenously.