CDK12-IN-4


Catalog No. Size PriceQuantity
M17482-C Contact sales@xcessbio.com for quotation $100

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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