212844-53-6 Usage
Description
Purvalanol A (212844-53-6) is a cyclin-dependent kinase inhibitor. IC50s= 4, 70, 35, 75 and 850 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk5/p35 and cdk4/cyclin D1 and respectively.1?Reversibly arrests synchronized cells in G1 and G2 phase.2?Induces ER stress-mediated apoptosis and autophagy in colon cancer cells.3?Suppresses Src-mediated transformation by inhibiting both CDKs and c-Src.4?In cells transformed with MYC, purvalanol A rapidly down-regulates survivin expression and induces MYC-dependent apoptosis.5?Cell permeable.
Uses
Purvalanol A acts as a potent, cell-permeable CDK inhibitor used in the treatment of cell proliferative disorders. Anti-cancer.
Biological Activity
Cyclin-dependent kinase inhibitor. IC 50 values are 4, 70, 35, 850 and 75 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively. Reversibly arrests synchronised cells in G1 and G2, and inhibits cell proliferation and cell death.
References
1) Gray?et al.?(1998),?Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors; Science,?281?533
2) Villerbu?et al.?(2002),?Cellular effects of purvalanol A: a specific inhibitor of cyclin-dependent kinase activities; Int. J. Cancer,?97?761
3) Coker-Gurkan?et al.?(2015),?Purvalanol induces endoplasmic reticulum stress-mediated apoptosis and autophagy in a time dependent manner in HCT116 colon cancer cells; Oncol. Rep.,?33?2761
4) Hikita?et al.?(2010),?Purvalanol A, a CDK inhibitor, effectively suppresses Src-mediated transformation by inhibiting both CDKs and c-Src; Genes Cells,?15?1051
5) Goga?et al.?(2007),?Inhibition of CDK1 as a potential therapy for tumors over-expressing MYC; Nat. Med.,?13?820
Check Digit Verification of cas no
The CAS Registry Mumber 212844-53-6 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,1,2,8,4 and 4 respectively; the second part has 2 digits, 5 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 212844-53:
(8*2)+(7*1)+(6*2)+(5*8)+(4*4)+(3*4)+(2*5)+(1*3)=116
116 % 10 = 6
So 212844-53-6 is a valid CAS Registry Number.
InChI:InChI=1/C19H25ClN6O/c1-11(2)15(9-27)23-19-24-17(22-14-7-5-6-13(20)8-14)16-18(25-19)26(10-21-16)12(3)4/h5-8,10-12,15,27H,9H2,1-4H3,(H2,22,23,24,25)/t15-/m0/s1
212844-53-6Relevant articles and documents
Oxidative amination of cuprated pyrimidine and purine derivatives
Boudet, Nadege,Dubbaka, Srinivas Reddy,Knochel, Paul
supporting information; experimental part, p. 1715 - 1718 (2009/04/10)
Using regioselective cuprations (via magnesiations), various primary, secondary and tertiary aminated pyrimidine and purine derivatives were prepared by the oxidative coupling of lithium amidocuprates using chloranil. DNA and RNA units such as aminated uracil or thymine, and adenine, as well as a CDK inhibitor, purvalanol A, were all obtained under mild conditions and satisfactory yields.
