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Pamufetinib mesylate

Catalog No. T13108L CAS 1688673-09-7

Synonyms: TAS-115 methanesulfonate, TAS-115 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).

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Pamufetinib mesylate, CAS 1688673-09-7

Pack Size	Availability	Price/USD	Quantity
1 mg	5 days	$ 67.00
5 mg	5 days	$ 197.00

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

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	rVEGFR2:30 nM , rMET:32 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].

Synonyms	TAS-115 methanesulfonate, TAS-115 mesylate
Molecular Weight	614.66
Formula	C28H27FN4O7S2
CAS No.	1688673-09-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

Solubility Information

DMSO: 75 mg/mL (122.02 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Fujita H, et al. The novel VEGF receptor/MET-targeted kinase inhibitor TAS-115 has marked in vivo antitumor properties and a favorable tolerability profile. Mol Cancer Ther. 2013 Dec;12(12):2685-96. 2. Nakade J, et al. Triple inhibition of EGFR, Met, and VEGF suppresses regrowth of HGF-triggered, erlotinib-resistant lung cancer harboring an EGFR mutation. J Thorac Oncol. 2014 Jun;9(6):775-83.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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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

Pamufetinib mesylate 1688673-09-7 Others TAS-115 methanesulfonate TAS-115 mesylate inhibitor inhibit

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