Cdk/Crk InhibitorCAS: 784211-09-2
MF: C23H22Cl2N4O3
MW: 473.4
A pyrazolo-pyrimidinone compound that acts as a potent, selective & ATP-competitive inhibitor of Cdks.

Cdk/Crk Inhibitor (CAS 784211-09-2)

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Synonym: 1-(2,6-Dichlorophenyl)-1,5-dihydro-6-((4-(2-hydroxyethoxy)phenyl)methyl)-3-(1-methylethyl)-4H-pyrazolo[3,4-d]pyrimidin-4-one; RGB-286147; Cdk7 Inhibitor IV
Application: A pyrazolo-pyrimidinone compound that acts as a potent, selective & ATP-competitive inhibitor of Cdks
CAS Number: 784211-09-2
Purity: >95%
Molecular Weight: 473.4
Molecular Formula: C23H22Cl2N4O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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Cdk/Crk Inhibitor is a cell-permeable pyrazolo-pyrimidinone compound that acts as a potent, selective, and ATP-competitive inhibitor of Cdks (IC50 = 48 nM, 15 nM, 9 nM, 10 nM, 71 nM, and 9 nM for Cdc2 (Cdk1)/cyclin B, Cdk2/cyclin E, Cdk3/cyclin E, Cdk5/p35, Cdk7/cyclin H/MAT1, and Cdk9, respectively). It inhibits Cdk4/cyclin D1, Cdk6/cyclin D3, and GSK-3β only at much higher concentrations (IC50 = 839 nM, 282 nM, and 754 nM, respectively) and exhibits little activity towards a panel of 60 other kinases. Cdk/Crk Inhibitor is a broad-spectrum growth inhibitor toward tumor cells, but not non-transformed quiescent fibroblasts.


References

Caligiuri, M., et al. 2005. Chem. Biol. 12, 1103.

Physical State :
Solid
Solubility :
Soluble in DMSO (5 mg/ml).
Storage :
Store at -20° C
IC50 :
Cdk1/B: IC50 = 48 nM; Cdk2/E: IC50 = 15 nM; Cdk3/E: IC50 = 9 nM; Cdk5/p35: IC50 = 10 nM; Cdk7/H/MAT1: IC50 = 71 nM; Cdk9: IC50 = 9 nM; Cdk4/D1: IC50 = 839 nM; Cdk6/D3: IC50 = 282 nM; GSK-3β: IC50 = 754 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
9549301
SMILES :
CC(C)C1=C2C(=NC(=NC2=O)CC3=CC=C(C=C3)OCCO)N(N1)C4=C(C=CC=C4Cl)Cl

Download SDS (MSDS)

Certificate of Analysis

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