WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 206184
CAS#: 895519-90-1 (free base)
Description: 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#: 206184
Name: Flumatinib free base
CAS#: 895519-90-1 (free base)
Chemical Formula: C29H29F3N8O
Exact Mass: 562.24164
Molecular Weight: 562.59
Elemental Analysis: C, 61.91; H, 5.20; F, 10.13; N, 19.92; O, 2.84
Flumatinib free base, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.
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/h3-9,14-17H,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
The following data is based on the product molecular weight 562.59 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: 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; PubMed Central PMCID: PMC4317885.
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.
Related CAS#
CAS No.
895519-90-1 (Flumatinib)
895519-91-2 (Flumatinib Mesylate)
