storage temp. :Store at +4°C solubility :DMSO: ~17 mg/mL form :crystalline color :brown
Safety Information
Symbol(GHS):
Signal word:
Warning
Hazard statements:
Code
Hazard statements
Hazard class
Category
Signal word
Pictogram
P-Codes
H302
Harmful if swallowed
Acute toxicity,oral
Category 4
Warning
P264, P270, P301+P312, P330, P501
H315
Causes skin irritation
Skin corrosion/irritation
Category 2
Warning
P264, P280, P302+P352, P321,P332+P313, P362
H319
Causes serious eye irritation
Serious eye damage/eye irritation
Category 2A
Warning
P264, P280, P305+P351+P338,P337+P313P
H335
May cause respiratory irritation
Specific target organ toxicity, single exposure;Respiratory tract irritation
Category 3
Warning
Precautionary statements:
P261
Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338
IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
Description
SU 9516 is a 3-substituted indolinone that has anti-proliferative and pro-apoptotic activity in tumor cells. It is a potent inhibitor of several cyclin-dependent kinases (CDKs) with selectivity for Cdk2 (IC50s = 22, 40, and 200 nM for Cdk2/cyclin A, Cdk1/cyclin B, and Cdk4/cyclin D1). It does not inhibit PKC, p38, PDGFR, or EGFR (IC50’s = >10 μM). SU 9516 inhibits phosphorylation of the retinoblastoma protein pRb, resulting in increased pRb/E2F complex formation, cell-cycle arrest, and subsequent apoptosis. In leukemia cells (U937, Jurkat, and HL-60 cells) SU 9516 downregulates transcription of the antiapoptotic protein Mcl-1, leading to mitochondrial injury and cell death.
