CDK12-IN-5

Modify Date: 2024-01-20 15:32:53

CDK12-IN-5 Structure
CDK12-IN-5 structure
Common Name CDK12-IN-5
CAS Number 2651200-35-8 Molecular Weight 454.36
Density N/A Boiling Point N/A
Molecular Formula C18H15F5N8O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of CDK12-IN-5


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].

 Names

Name CDK12-IN-5

 CDK12-IN-5 Biological Activity

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].
Related Catalog
Target

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].
References

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

 Chemical & Physical Properties

Molecular Formula C18H15F5N8O
Molecular Weight 454.36
Top Suppliers:I want be here

Get all suppliers and price by the below link:

CDK12-IN-5 suppliers

CDK12-IN-5 price