CTX-439
CTX-439 is an orally active, ATP-competitive small-molecule inhibitor of CDK12 and CDK13, with an IC50 of 3.1 nM and a Kd of 0.38 nM against CDK12, and an IC50 of 9.2 nM against CDK13. CTX-439 induces DNA damage and apoptosis in tumor cells. CTX-439 is applicable for the research of breast cancer and ovarian cancer.
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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: 2377487-13-1
- 分子式: C30H32F3N9O4S
- 分子量:671.69
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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
CTX-439 (0-10 μM; 6-72 h) inhibits the proliferation of SUM149PT cells with an IC50 of 100.5 nM, induces DNA damage and apoptosis, and downregulates the expression of DNA damage repair genes by inhibiting CDK12 activity[1].
CTX-439 (0-1 μM; 0-24 h) downregulates MCL1 protein levels in SUM149PT and OV90 cells[1].
CTX-439 (100-800 nM; 4-8 h) synergizes with the BCL-2/BCL-xL inhibitor AZD4320 (HY-112416) to rapidly induce apoptosis in SUM149PT and OV90 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/cA Jcl-nu/nu (6-week-old, nude, subcutaneous injection of 3 × 106 SUM149PT cells)[1]
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Dosage:7.5 mg/kg; 15 mg/kg; 30 mg/kg
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Administration:i.g.; twice weekly; 15 days
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Result:Significantly suppressed tumor growth.
Caused tumor regression.
Did not cause significant weight loss at any dose.
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Animal Model:BALB/cA Jcl-nu/nu (6-week-old, nude, subcutaneous injection of 3 × 106 SUM149PT cells)[1]
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Dosage:7.5 mg/kg
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Administration:i.g.; twice weekly; 15 days
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Result:Significantly suppressed tumor growth relative to vehicle, with final tumor volumes lower than vehicle but higher than combination treatment.
Downregulated MCL1 protein levels, reduced CDK12 S423 phosphorylation, and induced cleaved PARP and cleaved Caspase-3 levels in tumor tissue.
Did not cause significant weight loss.
化学情報
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CAS 番号 2377487-13-1
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分子量 671.69
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分子式 C30H32F3N9O4S
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SMILES
O=C(CCC)N(C1=CN=C(C2=CN=C(OC)N=C2)C=N1)[C@@H]3CC[C@@H](NC4=NC(C5=CC(S(C)(=O)=O)=CN=C5)=C(C(F)(F)F)C=N4)CC3
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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)
CTX-439 関連分類
HY-182312 関連分類
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