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CDK12-IN-5

Catalog No. T40290 CAS 2651200-35-8

Synonyms: CDK12-IN-5

CDK12-IN-5 is a pyrazolotriazine compound that effectively inhibits CDK12, with an IC50 value of 23.9 nM at a high ATP concentration of 2 mM. However, CDK12-IN-5 does not exhibit inhibitory effects on CDK2/Cyclin E (IC50 = 173 μM) and CDK9/Cyclin T1 (IC50 = 127 μM) at the same high ATP concentration of 2 mM, as stated in WO2021116178A1.

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CDK12-IN-5, CAS 2651200-35-8

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Description	CDK12-IN-5 is a pyrazolotriazine compound that effectively inhibits CDK12, with an IC50 value of 23.9 nM at a high ATP concentration of 2 mM. However, CDK12-IN-5 does not exhibit inhibitory effects on CDK2/Cyclin E (IC50 = 173 μM) and CDK9/Cyclin T1 (IC50 = 127 μM) at the same high ATP concentration of 2 mM, as stated in WO2021116178A1.
Targets&IC50	CDK12:23.9 nM (IC50), CDK2-CyclinE:173 μM (IC50), CDK9-CyclinT1:127 μM (IC50)
In vitro	CDK12-IN-5 (Example 426) selectively suppresses BRCA1 mRNA levels in MDA-MB-231 cells (IC50 = 3.23 nM) without affecting CAL-120 cells[1]. It exhibits antiproliferative effects on both MDA-MB-231 (IC50 = 4.19 nM) and CAL-120 cells (IC50 = 3.57 nM)[1]. Additionally, CDK12-IN-5 demonstrates a high selectivity for CDK12 inhibition with an IC50 to degradation (DC50) CDK12 ratio of 32[1].

Synonyms	CDK12-IN-5
Molecular Weight	454.365
Formula	C18H15F5N8O
CAS No.	2651200-35-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Kai Thede, et al. Pyrazolotriazines. WO2021116178A1.

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Keywords

CDK12-IN-5 2651200-35-8 CDK-12-IN-5 CDK12IN5 CDK12 IN 5 inhibitor inhibit

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