XL-281

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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 204730

CAS#: 870603-16-0

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.


Chemical Structure

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XL-281
CAS# 870603-16-0

Theoretical Analysis

MedKoo Cat#: 204730
Name: XL-281
CAS#: 870603-16-0
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

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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

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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

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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.



Additional Information