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Pamufetinib mesylate

Pamufetinib mesylate
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).
Catalog No. T13108LCas No. 1688673-09-7

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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).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
2 mg$955 days
5 mg$1975 days
50 mg$7471-2 weeks
100 mg$1,2401-2 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).
Targets&IC50
MET (rat):32 nM , VEGFR2 (rat):30 nM
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].
AliasTAS-115 mesylate, TAS-115 methanesulfonate
Chemical Properties
Molecular Weight614.66
FormulaC28H27FN4O7S2
Cas No.1688673-09-7
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 75 mg/mL (122.02 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.6269 mL8.1346 mL16.2692 mL81.3458 mL
5 mM0.3254 mL1.6269 mL3.2538 mL16.2692 mL
10 mM0.1627 mL0.8135 mL1.6269 mL8.1346 mL
20 mM0.0813 mL0.4067 mL0.8135 mL4.0673 mL
50 mM0.0325 mL0.1627 mL0.3254 mL1.6269 mL
100 mM0.0163 mL0.0813 mL0.1627 mL0.8135 mL

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