SU 9516

Product NameSU 9516
CAS377090-84-1
MFC13H11N3O2
MW241.25
EINECS
MOL File377090-84-1.mol

Chemical Properties

Boiling point	601.521±55.00 °C(Press: 760.00 Torr)(predicted)
Density	1.383±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted)
storage temp.	Store at +4°C
solubility	DMSO: ~17 mg/mL
pka	12.195±0.10(predicted)
form	crystalline
color	brown

Safety Information

Safety Statements	22-24/25
WGK Germany	3

Usage And Synthesis

Uses

SU 9516 is a 3-substituted indolinone CDK inhibitor with potent and selective inhibition towards cyclin-dependant kinases.

Definition

ChEBI: 3-(1H-imidazol-5-ylmethylidene)-5-methoxy-1H-indol-2-one is a member of indoles.

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 .

IC 50

CDK2: 22 nM (IC₅₀); CDK1: 40 nM (IC₅₀); CDK4: 200 nM (IC₅₀); PDGFr: 18000 nM (IC₅₀)

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.