CAS
377090-84-1
Formulation
A crystalline solid
Purity
≥98%
MW
241,3
Shipment
-20
Long Term Storage
-20
Shelf Life
1460
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).{23507} It does not inhibit PKC, p38, PDGFR, or EGFR (IC50s = >10 µM).{23507} SU 9516 inhibits phosphorylation of the retinoblastoma protein pRb, resulting in increased pRb/E2F complex formation, cell-cycle arrest, and subsequent apoptosis.{23507,23508} 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.{23509}
ESCLUSIVAMENTE PER USO DI RICERCA (RUO) e non per uso terapeutico o diagnostico su uomini o animali. Il prodotto NON è un Dispositivo Medico o un Diagnostico in Vitro.
PRODUCT FOR RESEARCH USE ONLY (RUO) and not for therapeutic or diagnostic use on humans or animals. The product is NOT a Medical Device or an In-Vitro Diagnostic (IVD).