Sitravatinib (Synonyms: MGCD-516) |
| Catalog No.GC19332 |
Le sitravatinib (MGCD516) est un inhibiteur du récepteur tyrosine kinase (RTK) biodisponible par voie orale avec des CI50 de 1,5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0,5 nM, 29 nM, 5 nM et 9 nM pour Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectivement .
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1123837-84-2
Sample solution is provided at 25 µL, 10mM.
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Sitravatinib is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth with IC50 of 3980 nmol/Lin vitro: MGCD516 is superior to other multi-kinase inhibitors in inhibiting cell proliferation, RTK phosphorylation, and phosphorylation of downstream effectors. MGCD516 is unique in a way that it has broad spectrum activity against many RTKs including c-Met, c-Kit, Axl, PDGFR, and Eph receptors that are known to play a role in driving sarcoma cell growthIn vivo: MGCD516 induces significant tumor growth suppression than imatinib and crizotinib.
References:
[1]. Patwardhan PP et al. Significant blockade of multiple receptor tyrosine kinases by MGCD516 (Sitravatinib), a novel small molecule inhibitor, shows potent anti-tumor activity in preclinical models of sarcoma. Oncotarget, 2016 Jan 26;7(4):4093-109.
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)
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