Description
CDK12-IN-4, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 0.641 μM at high ATP (2 mM). CDK12-IN-4 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1).
Product information
CAS Number: 2651196-69-7
Molecular Weight: 426.42
Formula: C20H20F2N8O
Chemical Name: 8-cyclopropyl-N-((6, 7-difluoro-1H-benzo[d]imidazol-2-yl)methyl)-2-morpholinopyrazolo[1, 5-a][1, 3, 5]triazin-4-amine
Smiles: FC1=C2NC(CNC3=NC(=NC4=C(C=NN34)C3CC3)N3CCOCC3)=NC2=CC=C1F
InChiKey: UXJVUCJEHIXDPU-UHFFFAOYSA-N
InChi: InChI=1S/C20H20F2N8O/c21-13-3-4-14-17(16(13)22)26-15(25-14)10-23-19-28-20(29-5-7-31-8-6-29)27-18-12(11-1-2-11)9-24-30(18)19/h3-4,9,11H,1-2,5-8,10H2,(H,25,26)(H,23,27,28)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
CDK12-IN-4 (Example 172) inhibits BRCA1 MRNA expression in MDA-MB-231 cells (IC50=0.626 nM) and has no effect on CAL-120 cells. CDK12-IN-4 has antproliferative activity in MDA-MB-231 cells (IC50=0.535 nM) and CAL-120 cells (IC50=2.43 nM). CDK12-IN-4 has a inhibition IC50 CDK12 high ATP to Degradation DC50 CDK12 ratio of 581.
Products are for research use only. Not for human use.
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