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Product name : Lee011
Item : CR1779
Price : 100mg, $945; 200mg, $1485
contact : Send inquiry to: info@acesobio.com
Additional Information :  We offer significant discount for bulky quantity order,Please ask price and availability of other quantities
CAS : 1256963-02-6
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Details:
 Chemical Information
M.Wt 440.97 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C22H29ClN8
CAS No 1256963-02-6
Solubility

DMSO



Biological Activity of CDK4-IN-1

 

CDK4 inhibitor is a novel and specific CDK4/Cyclin D1 inhibitor with an IC50 of 10 nM; 1500 and 500 fold than CDK1/Cyclin B (IC50>15 uM) and CDK2/Cyclin A (IC50=5.265 uM) respectively.
IC50 Value: 10 nM (CDK4/Cyclin D1) [1]
Target: CDK4
CDK4/6 inhibitor imposed a G1 block on cells at 0.37μM in the CDK4 Cellular Assays. CDK4/6 inhibitor exhibited the most sustained G1 arrest among five compounds and were tested further against a selection of serine-threonine and tyrosine kinases and proved to be selective for CDK4/6 over 35 other kinases [1].
 

 

[1]. Cho YS, et al. 4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6. J Med Chem. 2010 Nov 25;53(22):7938-57.
Abstract
Identification and structure-guided optimization of a series of 4-(pyrazol-4-yl)-pyrimidines as selective CDK4/6 inhibitors is reported herein. Several potency and selectivity determinants were established based on the X-ray crystallographic analysis of representative compounds bound to monomeric CDK6. Significant selectivity for CDK4/6 over CDK1 and CDK2 was demonstrated with several compounds in both enzymatic and cellular assays.


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