1. Cell Cycle/DNA Damage
  2. CDK
  3. CDK12-IN-5

CDK12-IN-5 

Cat. No.: HY-139328
Handling Instructions

CDK12-IN-5, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 23.9 nM at high ATP (2 mM). CDK12-IN-5 has no effect on CDK2/Cyclin E (IC50=173 μM) and CDK9/Cyclin T1 (IC50=127 μM) at high ATP (2 mM) (WO2021116178A1).

For research use only. We do not sell to patients.

CDK12-IN-5 Chemical Structure

CDK12-IN-5 Chemical Structure

CAS No. : 2651200-35-8

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Description

CDK12-IN-5, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 23.9 nM at high ATP (2 mM). CDK12-IN-5 has no effect on CDK2/Cyclin E (IC50=173 μM) and CDK9/Cyclin T1 (IC50=127 μM) at high ATP (2 mM) (WO2021116178A1)[1].

IC50 & Target[1]

CDK12

23.9 nM (IC50)

CDK2/cyclinE

173 μM (IC50)

CDK9/cyclinT1

127 μM (IC50)

In Vitro

CDK12-IN-5 (Example 426) inhibits BRCA1 MRNA expression in MDA-MB-231 cells (IC50=3.23 nM) and has no effect on CAL-120 cells[1].
CDK12-IN-5 has antproliferative activity in MDA-MB-231 cells (IC50=4.19 nM) and CAL-120 cells (IC50=3.57 nM)[1].
CDK12-IN-5 has a inhibition IC50 CDK12 high ATP to Degradation DC50 CDK12 ratio of 32[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

454.36

Formula

C₁₈H₁₅F₅N₈O

CAS No.
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Storage

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CDK12-IN-5
Cat. No.:
HY-139328
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