377090-84-1 Usage
Description
SU 9516 is a 3-substituted indolinone CDK inhibitor, which demonstrates potent and selective inhibition towards cyclin-dependent kinases (CDKs). These kinases play a crucial role in regulating cell cycle progression, and their dysregulation has been implicated in various diseases, including cancer.
Uses
Used in Pharmaceutical Industry:
SU 9516 is used as a CDK inhibitor for its potential application in cancer treatment. By selectively inhibiting CDKs, SU 9516 can interfere with the cell cycle, thereby preventing the uncontrolled cell division and growth associated with cancer. This targeted approach may offer a more effective and less toxic alternative to conventional chemotherapy.
Additionally, SU 9516's ability to inhibit CDKs could make it a valuable tool in the development of new therapeutic strategies for other diseases where CDK dysregulation is a factor, such as neurodegenerative disorders or cardiovascular diseases. Further research and clinical trials would be necessary to explore these potential applications.
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-