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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- No. CAS: 2377487-13-1
- Fòrmula: C30H32F3N9O4S
- Peso molecular:671.69
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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.
Chemical Information
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No. CAS 2377487-13-1
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Peso molecular 671.69
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CTX-439 Related Classifications
HY-182312 Related Classifications
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