CDK12-IN-4
CDK12-IN-4, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 0.641 μM at high ATP (2 mM). CDK12-IN-4 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1).
For research use only. We do not sell to patients.
- CAS No.: 2651196-69-7
- Formula: C20H20F2N8O
- Molecular Weight:426.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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CDK12 0.641 μM (IC50) |
CDK2/cyclinE >20 μM (IC50) |
CDK9/cyclinT1 >20 μM (IC50) |
CDK12-IN-4 (Example 172) inhibits BRCA1 MRNA expression in MDA-MB-231 cells (IC50=0.626 nM) and has no effect on CAL-120 cells[1].
CDK12-IN-4 has antproliferative activity in MDA-MB-231 cells (IC50=0.535 nM) and CAL-120 cells (IC50=2.43 nM)[1].
CDK12-IN-4 has a inhibition IC50 CDK12 high ATP to Degradation DC50 CDK12 ratio of 581[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2651196-69-7
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Molecular Weight 426.42
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Formula C20H20F2N8O
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SMILES
FC1=C(F)C2=C(N=C(CNC3=NC(N4CCOCC4)=NC5=C(C6CC6)C=NN35)N2)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDK12-IN-4 Related Classifications
HY-139327 Related Classifications
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