Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CDK12-IN-6, a pyrazolotriazine compound, is a powerful inhibitor of CDK12. Its inhibitory activity is significant with an IC50 value of 1.19 μM when tested at high ATP concentration (2 mM). Notably, CDK12-IN-6 does not exhibit any inhibitory effect on CDK2/Cyclin E (IC50 <20 μM) and CDK9/Cyclin T1 (IC50 <20 μM) when tested under the same high ATP conditions (2 mM) (WO2021116178A1).
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Description | CDK12-IN-6, a pyrazolotriazine compound, is a powerful inhibitor of CDK12. Its inhibitory activity is significant with an IC50 value of 1.19 μM when tested at high ATP concentration (2 mM). Notably, CDK12-IN-6 does not exhibit any inhibitory effect on CDK2/Cyclin E (IC50 >20 μM) and CDK9/Cyclin T1 (IC50 >20 μM) when tested under the same high ATP conditions (2 mM) (WO2021116178A1). |
Targets&IC50 | CDK12:1.19 μM (IC50), CDK2-CyclinE:>20 μM (IC50), CDK9-CyclinT1:>20 μM (IC50) |
In vitro | CDK12-IN-6 (Example 174) suppresses BRCA1 mRNA expression in MDA-MB-231 cells with an IC 50 value of 0.872 nM, while having no impact on CAL-120 cells. Additionally, it demonstrates antiproliferative effects in both MDA-MB-231 (IC 50 = 2.19 nM) and CAL-120 cells (IC 50 = 1 nM). Furthermore, CDK12-IN-6 exhibits a high CDK12 inhibition efficiency with an IC 50 to DC 50 ratio of 1851, indicating its potent activity in hindering CDK12 in the context of ATP to degradation processes. |
Synonyms | CDK12-IN-6 |
Molecular Weight | 425.448 |
Formula | C20H21F2N9 |
CAS No. | 2651196-71-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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CDK12-IN-6 2651196-71-1 CDK12 IN 6 CDK-12-IN-6 CDK12IN6 inhibitor inhibit