377090-84-1 Usage
Uses
SU 9516 is a 3-substituted indolinone CDK inhibitor with potent and selective inhibition towards cyclin-dependant kinases.
Biological Activity
Potent, selective cdk2 inhibitor (IC 50 values are 0.022, 0.04, >10, >10, 18 and >100 μ M for cdk2, cdk1, cdk4, PKC, p38, PDGFR and EGFR respectively). Inhibits pRb phosphorylation causing enhanced pRB/E2F complex formation and induces G 1 and G 2 -M cell cycle arrest. Transcriptionally downregulates Mcl-1 and has antiproliferative, cytostatic and pro-apoptotic effects in vitro .
references
[1]. lane me, yu b, rice a, et al. a novel cdk2-selective inhibitor, su9516, induces apoptosis in colon carcinoma cells. cancer res, 2001, 61(16): 6170-6177.[2]. yu b, lane me, wadler s. su9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight e2f complexes in human colon carcinoma cells. biochem pharmacol, 2002, 64(7): 1091-1100.[3]. gao n, kramer l, rahmani m, et al. the three-substituted indolinone cyclin-dependent kinase 2 inhibitor 3-[1-(3h-imidazol-4-yl)-meth-(z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one (su9516) kills human leukemia cells via down-regulation of mcl-1 through a transcriptional mechanism. mol pharmacol, 2006, 70(2): 645-655.
Check Digit Verification of cas no
The CAS Registry Mumber 377090-84-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,7,7,0,9 and 0 respectively; the second part has 2 digits, 8 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 377090-84:
(8*3)+(7*7)+(6*7)+(5*0)+(4*9)+(3*0)+(2*8)+(1*4)=171
171 % 10 = 1
So 377090-84-1 is a valid CAS Registry Number.
InChI:InChI=1/C13H11N3O2/c1-18-9-2-3-12-10(5-9)11(13(17)16-12)4-8-6-14-7-15-8/h2-7H,1H3,(H,14,15)(H,16,17)/b11-4-
