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
XL-281 is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to firstname.lastname@example.org to inquire quote.
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
The following data is based on the product molecular weight 462.89 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
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.