CB 3703
CB 3703 is an inhibitor of thymidylate synthase (TS) and dihydrofolate reductase (DHFR). CB 3703 has an IC50 of 0.25 μM against rat TS, a Ki of 0.47 μM against mouse TS, an IC50 of 6.8 nM against rat DHFR, and a Ki of 0.6 pM against mouse DHFR. CB 3703 is transported via the reduced folate pathway, has a short plasma half-life, and can prolong the survival of tumor-bearing mice. CB 3703 can be used in the research of L1210 ascites tumors.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 32093-09-7
- 分子式: C22H24N6O5
- 分子量:452.46
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| L1210 | IC50 |
0.019 μM
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Growth inhibition against mouse L1210 cells assessed as reduction in cell count after 48 hr incubation.
Growth inhibition against mouse L1210 cells assessed as reduction in cell count after 48 hr incubation.
|
0014296480902145 |
体外実験
CB 3703 (6.8 nM-100 μM) potently inhibits rat liver DHFR (I50=6.8 nM) and Yoshida ascites sarcoma TS (I50=0.25 μM), and weakly inhibits other folate metabolizing enzymes at 100 μM[1].
CB 3703 potently inhibits purified L1210 cell DHFR (Ki=0.6 pM, competitive) and purified L1210 cell TS (Ki=0.47 μM, non-competitive), and weakly inhibits rat liver methionine synthetase (Ki=0.36 mM)[1].
CB 3703 (50 nM; 48 hr) toxicity to L1210 cells is partially reversed by thymidine or folinic acid alone, improved by their combination, and fully reversed only by thymidine plus hypoxanthine[1].
CB 3703 (0.019 μM; 48 hr) inhibits L1210 cell growth with an I50 of 0.019 μM[1].
CB 3703 (2-40 μM; 20 min) competes with methotrexate for uptake into L1210 cells, and weakly competes with folic acid, suggesting shared transport pathways[1].
CB 3703 (4 μM; 0-40 min) accumulates to ~10-fold higher intracellular levels than methotrexate in L1210 cells over 40 minutes, does not plateau within this time, and does not use the folic acid transport pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:L1210 cells
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Concentration:0.019 μM
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Incubation Time:48 hr
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Result:Reduced L1210 cell count to 50% of control levels after 48 hr incubation at 0.019 μM.
Parmacokinetics
| Species | Dose | Route | T1/2 | Plasma Concentration |
|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.p. | 1.54 h | 0.05 μM |
体内実験
CB 3703 (1-8 mg/kg; i.p.; single dose) has an LD50 between 2 mg/kg and 4 mg/kg in healthy female (DBA2×C57B1)F1 mice following a single i.p. dose[1].
CB 3703 (10 mg/kg; i.p.; single dose) exhibits a plasma half-life of 1.54 hours in healthy female (DBA2×C57B1)F1 mice following a single 10 mg/kg i.p. dose, with barely detectable levels at 24 hours[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:(DBA2×C57B1)F1 hybrid (9-12-week-old female; L1210 leukaemia ascites model, injected i.p. with 5×104 tumour cells 3 days prior to treatment)[1]
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Dosage:1 mg/kg; 2 mg/kg; 4 mg/kg; 8 mg/kg
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Administration:i.p.; single dose
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Result:Produced a 36% increase in median survival time (from 14 days in untreated controls to 19 days).
Produced a 64% increase in median survival time (to 23 days).
Caused 3/5 tumour-bearing mice to die from toxicity before 10 days.
Caused all 5 tumour-bearing mice to die from toxicity before 10 days.
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Animal Model:(DBA2×C57B1)F1 hybrid (9-12-week-old female; healthy, non-tumour bearing)[1]
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Dosage:1 mg/kg; 2 mg/kg; 4 mg/kg; 8 mg/kg
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Administration:i.p.; single dose
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Result:Caused 5/11 mice to die from toxicity.
Caused 1/10 mice to die from toxicity.
Caused all 10 mice to die from toxicity.
Caused all 10 mice to die from toxicity.
Resulted in an LD50 between 2 mg/kg and 4 mg/kg.
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Animal Model:(DBA2×C57B1)F1 hybrid (9-12-week-old female; healthy, non-tumour bearing)[1]
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Dosage:10 mg/kg
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Administration:i.p.; single dose
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Result:Exhibited exponential plasma level decay over the first 8 hours with a half-life of 1.54 hours.
Reached barely detectable plasma levels of approximately 0.05 μM at 24 hours.
化学情報
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CAS 番号 32093-09-7
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分子量 452.46
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分子式 C22H24N6O5
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SMILES
O=C(O)CC[C@@H](C(O)=O)NC(C1=CC=C(NCC2=C(C)C3=C(N)N=C(N)N=C3C=C2)C=C1)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
CB 3703 関連分類
HY-119143 関連分類
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