WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 204730
Description: XL281, also known as BMS-908662 , is an orally active, small molecule Raf kinase inhibitor with potential antineoplastic activity. XL281 specifically inhibits RAF kinases, located downstream from RAS in the RAS/RAF/MEK/ERK kinase signaling pathway, which may result in reduced proliferation of tumor cells. RAS mutations may result in constitutive activation of the RAS/RAF/MEK/ERK kinase signaling pathway, and have been found to occur frequently in human tumors.
MedKoo Cat#: 204730
Chemical Formula: C24H19ClN4O4
Exact Mass: 462.10948
Molecular Weight: 462.89
Elemental Analysis: C, 62.27; H, 4.14; Cl, 7.66; N, 12.10; O, 13.83
Synonym: BMS908662; BMS-908662; BMS 908662; XL281; XL 281; XL-281
IUPAC/Chemical Name: methyl (5-(2-(5-chloro-2-methylphenyl)-1-hydroxy-3-oxoisoindolin-1-yl)-1H-benzo[d]imidazol-2-yl)carbamate
InChi Key: MMNNTJYFHUDSKL-UHFFFAOYSA-N
InChi Code: InChI=1S/C24H19ClN4O4/c1-13-7-9-15(25)12-20(13)29-21(30)16-5-3-4-6-17(16)24(29,32)14-8-10-18-19(11-14)27-22(26-18)28-23(31)33-2/h3-12,32H,1-2H3,(H2,26,27,28,31)
SMILES Code: O=C(OC)NC1=NC2=CC(C3(O)N(C4=CC(Cl)=CC=C4C)C(C5=C3C=CC=C5)=O)=CC=C2N1
1: Dickson MA, Gordon MS, Edelman G, Bendell JC, Kudchadkar RR, LoRusso PM, Johnston SH, Clary DO, Schwartz GK. Phase I study of XL281 (BMS-908662), a potent oral RAF kinase inhibitor, in patients with advanced solid tumors. Invest New Drugs. 2014 Dec 5. [Epub ahead of print] PubMed PMID: 25476894.
2: Belum VR, Rosen AC, Jaimes N, Dranitsaris G, Pulitzer MP, Busam KJ, Marghoob AA, Carvajal RD, Chapman PB, Lacouture ME. Clinico-morphological features of BRAF inhibition-induced proliferative skin lesions in cancer patients. Cancer. 2015 Jan 1;121(1):60-8. doi: 10.1002/cncr.28980. Epub 2014 Sep 3. PubMed PMID: 25186461.
3: Huang T, Karsy M, Zhuge J, Zhong M, Liu D. B-Raf and the inhibitors: from bench to bedside. J Hematol Oncol. 2013 Apr 25;6:30. doi: 10.1186/1756-8722-6-30. Review. PubMed PMID: 23617957; PubMed Central PMCID: PMC3646677.