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Flumatinib mesylate
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MedKoo CAT#: 206972

CAS#: 895519-91-2 (mesylate)

Description: Flumatinib, also known as HH-GV-678 , 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.


Price and Availability

Size Price Shipping out time Quantity
1g USD 150 2 Weeks
2g USD 250 2 Weeks
5g USD 450 2 Weeks
10g USD 850 2 Weeks
100g USD 2950 2 Weeks
200g USD 4950 2 Weeks
500g USD 9650 2 Weeks
Inquire bulk and customized quantity
Pricing updated 2020-07-09. Prices are subject to change without notice.

Flumatinib mesylate, 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.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 206972
Name: Flumatinib mesylate
CAS#: 895519-91-2 (mesylate)
Chemical Formula:
Exact Mass:
Molecular Weight:
Elemental Analysis:


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

Synonym: Flumatinib mesylate; 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 mesylate

InChi Key: ZSASDYCFROUKTJ-UHFFFAOYSA-N

InChi Code: InChI=1S/C29H29F3N8O.CH4O3S/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;1-5(2,3)4/h3-9,14-17H,10-13,18H2,1-2H3,(H,36,41)(H,34,37,38);1H3,(H,2,3,4)

SMILES Code: O=C(NC1=CC(NC2=NC=CC(C3=CC=CN=C3)=N2)=C(C)N=C1)C4=CC=C(CN5CCN(C)CC5)C(C(F)(F)F)=C4.OS(=O)(C)=O


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

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


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; 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.