Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CDK12-IN-4, a pyrazolotriazine compound, exhibits potent inhibition of CDK12 by achieving an IC50 value of 0.641 μM, utilizing high ATP levels (2 mM). Notably, CDK12-IN-4 does not impact CDK2/Cyclin E (IC50 < 20 μM) or CDK9/Cyclin T1 (IC50 < 20 μM) under the influence of high ATP (2 mM) levels (WO2021116178A1).
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Description | CDK12-IN-4, a pyrazolotriazine compound, exhibits potent inhibition of CDK12 by achieving an IC50 value of 0.641 μM, utilizing high ATP levels (2 mM). Notably, CDK12-IN-4 does not impact CDK2/Cyclin E (IC50 > 20 μM) or CDK9/Cyclin T1 (IC50 > 20 μM) under the influence of high ATP (2 mM) levels (WO2021116178A1). |
Targets&IC50 | CDK12:0.641 μM (IC50), CDK2-CyclinE:>20 μM (IC50), CDK9-CyclinT1:>20 μM (IC50) |
In vitro | CDK12-IN-4 (Example 172) selectively inhibits BRCA1 mRNA expression in MDA-MB-231 cells with an IC50 value of 0.626 nM, while not affecting CAL-120 cells. Additionally, it exhibits antiproliferative effects in both MDA-MB-231 and CAL-120 cells, with IC50 values of 0.535 nM and 2.43 nM, respectively. The compound also demonstrates a high CDK12 inhibition potency with an IC50 to degradation DC50 ratio of 581, indicating its effectiveness and selective action mechanism [1]. |
Synonyms | CDK12-IN-4 |
Molecular Weight | 426.432 |
Formula | C20H20F2N8O |
CAS No. | 2651196-69-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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CDK12-IN-4 2651196-69-7 CDK-12-IN-4 CDK12IN4 CDK12 IN 4 inhibitor inhibit