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Pamufetinib mesylate

Catalog No. T13108LCas No. 1688673-09-7

TAS-115 mesylate is a potent inhibitor of VEGFR and hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase(IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively).

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Pack Size	Price	Availability
2 mg	$95	5 days
5 mg	$197	5 days
50 mg	$747	1-2 weeks
100 mg	$1,240	1-2 weeks

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Product Introduction

Bioactivity

Description	TAS-115 mesylate is a potent inhibitor of VEGFR and hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase(IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively).
In vitro	TAS-115 powerfully suppresses the VEGF-dependent proliferation of HUVECs with IC50 of 0.019 μM as a VEGFR-targeted inhibitor and powerfully suppresses the proliferation of MET-amplified cancer cells with GI50 of 0.032-0.362 μM as a MET-targeted inhibitor. TAS-115 has much less toxicity in various normal cell lines when compared with other VEGFR-targeted kinase inhibitors[1].In PC-9 and HCC827 cells, Crizotinib and TAS-115 inhibit Met phosphorylation and reverse erlotinib resistance and VEGF production triggered by HGF [2].
In vivo	TAS-115 is administered daily for 6 weeks, and it can completely inhibit the progress of MET-inactivated tumors by blocking angiogenesis without toxicity, even at a serum-saturating dose of TAS-115. In MET-amplified human cancer–bearing mice, TAS-115 induces marked tumor shrinkage and prolonges survival [1].
Alias	TAS-115 mesylate, TAS-115 methanesulfonate

Chemical Properties

Molecular Weight	614.66
Formula	C28H27FN4O7S2
Cas No.	1688673-09-7

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 75 mg/mL (122.02 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.6269 mL	8.1346 mL	16.2692 mL	81.3458 mL
5 mM	0.3254 mL	1.6269 mL	3.2538 mL	16.2692 mL
10 mM	0.1627 mL	0.8135 mL	1.6269 mL	8.1346 mL
20 mM	0.0813 mL	0.4067 mL	0.8135 mL	4.0673 mL
50 mM	0.0325 mL	0.1627 mL	0.3254 mL	1.6269 mL
100 mM	0.0163 mL	0.0813 mL	0.1627 mL	0.8135 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

TAS115 MesylatePamufetinib mesylatePamufetinib MesylateTAS 115 MesylateTAS-115 Mesylate