Flumatinib, also known as HHGV678 , is a selective inhibitor of BCR-ABL/PDGFR/KIT. Flumatinib is currently in Phase I and II clinical trials in China for the treatment of chronic myelogenous leukemia (CML). Flumatinib effectively overcomes drug resistance of certain KIT mutants. Flumatinib mesylate can reduce the expression of C-MYC, HIF-1 α and VEGF in U266 cell line in a time- and dose-dependent manners.

MedKoo Cat#: 206184Name: FlumatinibCAS#: 895519-90-1 (free base)Chemical Formula: C29H29F3N8OExact Mass: 562.24164Molecular Weight: 562.59Elemental Analysis: C, 61.91; H, 5.20; F, 10.13; N, 19.92; O, 2.84

Related CAS #:895519-90-1 (free base)895519-91-2 (mesylate)

Synonym:HHGV678; HHGV 678 ; HHGV-678; HH-GV-678; Flumatinib;

IUPAC/Chemical Name:N-(6-methyl-5-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)pyridin-3-yl)-4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)benzamide

InChi Key:BJCJYEYYYGBROF-UHFFFAOYSA-N

InChi Code:InChI=1S/C29H29F3N8O/c1-19-26(38-28-34-9-7-25(37-28)21-4-3-8-33-16-21)15-23(17-35-19)36-27(41)20-5-6-22(24(14-20)29(30,31)32)18-40-12-10-39(2)11-13-40/h4-9,14-17H,10-13,18H2,1-2H3,(H,36,41)(H,34,37,38)

SMILES Code:CC1=C(NC2=NC=CC(C3=CN=CC=C3)=N2)C=C(NC(C4=CC(C(F)(F)F)=C(CN5CCN(C)CC5)C=C4)=O)C=N1

Technical Data

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).

Harmonized System Code:293490

Additional Information

Related CAS# CAS No. 895519-90-1 (Flumatinib) 895519-91-2 (Flumatinib Mesylate)      

References

1: Chang MX, Ma YP. [Effect of flumatinib mesylate on C-MYC, HIF-1α and VEGF in U226 line]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2013 Dec;21(6):1496-500. doi: 10.7534/j.issn.1009-2137.2013.06.024. Chinese. PubMed PMID: 24370036.

2: Zhao J, Quan H, Xu Y, Kong X, Jin L, Lou L. Flumatinib, a selective inhibitor of BCR-ABL/PDGFR/KIT, effectively overcomes drug resistance of certain KIT mutants. Cancer Sci. 2014 Jan;105(1):117-25. doi: 10.1111/cas.12320. Epub 2014 Jan 4. PubMed PMID: 24205792.

3: Yang Y, Liu K, Zhong D, Chen X. Simultaneous determination of flumatinib and its two major metabolites in plasma of chronic myelogenous leukemia patients by liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2012 May 1;895-896:25-30. doi: 10.1016/j.jchromb.2012.03.008. Epub 2012 Mar 15. PubMed PMID: 22472641.

4: Luo H, Quan H, Xie C, Xu Y, Fu L, Lou L. HH-GV-678, a novel selective inhibitor of Bcr-Abl, outperforms imatinib and effectively overrides imatinib resistance. Leukemia. 2010 Oct;24(10):1807-9. doi: 10.1038/leu.2010.169. Epub 2010 Aug 12. PubMed PMID: 20703259.

5: Gong A, Chen X, Deng P, Zhong D. Metabolism of flumatinib, a novel antineoplastic tyrosine kinase inhibitor, in chronic myelogenous leukemia patients. Drug Metab Dispos. 2010 Aug;38(8):1328-40. doi: 10.1124/dmd.110.032326. Epub 2010 May 17. PubMed PMID: 20478851.

6: Qiu L, Wang XD, Yu BH, Lu RZ, Ge F, Wang XL, Chen LJ, Han BH, Zhan ZM, Zhang BL, Ma J. [Effect of a novel tyrosine kinase inhibitor HHGV678 on growth inhibition of Bcr-Abl wild type and IM-resistant cell lines in vitro]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2008 Oct;16(5):1039-43. Chinese. PubMed PMID: 18928591.