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Flumatinib mesylate

CAS# 895519-91-2

Flumatinib mesylate

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Chemical structure

Flumatinib mesylate

3D structure

Chemical Properties of Flumatinib mesylate

Cas No. 895519-91-2 SDF Download SDF
PubChem ID 46910592 Appearance Powder
Formula C30H33F3N8O4S M.Wt 658.69
Type of Compound N/A Storage Desiccate at -20°C
Solubility H2O : 50 mg/mL (75.91 mM; Need ultrasonic)
DMSO : 50 mg/mL (75.91 mM; Need ultrasonic)
Chemical Name methanesulfonic acid;4-[(4-methylpiperazin-1-yl)methyl]-N-[6-methyl-5-[(4-pyridin-3-ylpyrimidin-2-yl)amino]pyridin-3-yl]-3-(trifluoromethyl)benzamide
SMILES CC1=C(C=C(C=N1)NC(=O)C2=CC(=C(C=C2)CN3CCN(CC3)C)C(F)(F)F)NC4=NC=CC(=N4)C5=CN=CC=C5.CS(=O)(=O)O
Standard InChIKey ZSASDYCFROUKTJ-UHFFFAOYSA-N
Standard InChI 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)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Flumatinib mesylate

DescriptionFlumatinib (HH-GV-678) ,a derivative of imatinib, is a multi-kinase inhibitor with IC50 Values of 1.2 nM, 307.6 nM and 2662 nM for c-Abl, PDGFRβ and c-Kit respectively.

Flumatinib mesylate Dilution Calculator

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Flumatinib mesylate Molarity Calculator

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Preparing Stock Solutions of Flumatinib mesylate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.5182 mL 7.5908 mL 15.1816 mL 30.3633 mL 37.9541 mL
5 mM 0.3036 mL 1.5182 mL 3.0363 mL 6.0727 mL 7.5908 mL
10 mM 0.1518 mL 0.7591 mL 1.5182 mL 3.0363 mL 3.7954 mL
50 mM 0.0304 mL 0.1518 mL 0.3036 mL 0.6073 mL 0.7591 mL
100 mM 0.0152 mL 0.0759 mL 0.1518 mL 0.3036 mL 0.3795 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Flumatinib mesylate

Flumatinib mesylate (HH-GV-678 mesylate), a derivative of imatinib, is a multi-kinase inhibitor with IC50 Values of 1.2 nM, 307.6 nM and 2662 nM for c-Abl, PDGFRβ and c-Kit respectively. IC50 Value: 1.2 nM (c-Abl); 307.6 nM(PDGFRβ); 2662 nM (c-Kit) [1] Target: c-Abl; c-Kit; PDGRFβ in vitro: HH-GV-678 can predominantly inhibit the autophosphorylation of Bcr-Abl in K562 cell. In higher concentration, HH-GV-678 can inhibit the phosphorylation of c-Kit in Mo7e cell and the phosphorylation of PDGFR in Swiss3T3 cell, however, HH-GV-678 has no or little effect on other tyrosine kinase including EGFR、KDR、c-Src andHER2 [1]. Flumatinib effectively overcame the drug resistance of certain KIT mutants with activation loop mutations (i.e., D820G, N822K, Y823D, and A829P) [2]. in vivo: The purpose of this study was to identify the metabolites of flumatinib in CML patients, with the aim of determining the main metabolic pathways offlumatinib in humans after oral administration. Ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry revealed 34 metabolites; 7 primary metabolites were confirmed by comparison with synthetic reference standards. The results show that the parent drugflumatinib was the main form recovered in human plasma, urine, and feces. The main metabolites of flumatinib in humans were the products of N-demethylation, N-oxidation, hydroxylation, and amide hydrolysis [3].

References:
[1]. Luo H, et al. HH-GV-678, a novel selective inhibitor of Bcr-Abl, outperforms imatinib and effectively overrides imatinib resistance. Leukemia. 2010 Oct;24(10):1807-9. [2]. Zhao J, et al. Flumatinib, a selective inhibitor of BCR-ABL/PDGFR/KIT, effectively overcomes drug resistance of certain KIT mutants. Cancer Sci. 2013 Nov 10. [3]. Gong A, et al. Metabolism of flumatinib, a novel antineoplastic tyrosine kinase inhibitor, in chronic myelogenous leukemia patients. Drug Metab Dispos. 2010 Aug;38(8):1328-40.

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References on Flumatinib mesylate

[Effect of flumatinib mesylate on C-MYC, HIF-1alpha and VEGF in U226 line].[Pubmed:24370036]

Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2013 Dec;21(6):1496-500.

The objective of this study was to investigate the effect of the new generation of tyrosine kinase inhibitor Flumatinib mesylate on C-MYC, HIF-1alpha and VEGF in multiple myeloma (MM) cell line U266. Different concentrations (1, 5, 10 micromol/L) of Flumatinib mesylate were used to act on U266 cell line for 8, 16 and 24 h, and the expression of C-MYC, and HIF-1alpha genes was detected by real-time fluorescence-quantitative PCR, the expression of C-MYC, HIF-1alpha and VEGF was measured by Western blot. The results showed that the gene expression of C-MYC and HIF-1 genes decreased gradually with the increasing of Flumatinib mesylate concentration (P < 0.05). At the same concentration of Flumatinib mesylate, the expression of C-MYC and HIF-1alpha gene decreased gradually with prolonging of treatment time with the Flumatinib mesylate (P < 0.05). When the Flumatinib mesylate acted the U266 cell line for 16 h, the expression of C-MYC, HIF-1alpha and VEGF decreased gradually with the increasing of Flumatinib mesylate concentration (P < 0.05). It is concluded that the Flumatinib mesylate can reduce the expression of C-MYC, HIF-1 alpha and VEGF in U266 cell line in a time- and dose-dependent manners, so Flumatinib mesylate may become a new drug for MM therapy.

Description

Flumatinib mesylate (HH-GV-678 mesylate), a derivative of imatinib, is a multi-kinase inhibitor with IC50 Values of 1.2 nM, 307.6 nM and 2662 nM for c-Abl, PDGFRβ and c-Kit respectively.

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