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Pamufetinib

Catalog No. T13108 CAS 1190836-34-0

Synonyms: H2OL3Q4XRD, 4-(2-Fluoro-4-(3-(2-phenylacetyl)thioureido)phenoxy)-7-methoxy-N-methylquinoline-6-carboxamide, TAS-115

Pamufetinib (TAS-115) 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, CAS 1190836-34-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 76.00
5 mg	In stock	$ 180.00
10 mg	In stock	$ 266.00
25 mg	In stock	$ 451.00
50 mg	In stock	$ 663.00
100 mg	In stock	$ 945.00
1 mL * 10 mM (in DMSO)	In stock	$ 226.00

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Purity: 99.15%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Pamufetinib (TAS-115) 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	c-Met:32 nM, VEGFR2:30 nM
In vitro	pamufetinib is ATP antagonism(Ki of 12 and 39 nM for rVEGFR2 and rMET, respectively). Like other known VEGFR or MET inhibitors, AS-115 strongly inhibits the kinase activity of VEGFR2 and MET and their signal-dependent cell growth. TAS-115 induces less damage in various normal cells than do other VEGFR inhibitors[1]. TAS-115 does not affect the growth of PC-9 or HCC827 cells at concentrations less than 10 μM; however, the combined use of TAS-115 with erlotinib reverses HGF-induced resistance in the cell lines in a concentration-dependent manner. VEGF production by cancer cells and endothelial proliferation inhibited by TAS-115[2].
In vivo	During the treatment period,pamufetinib (50 mg/kg/d) completely prevents tumor growth. In MET-amplified human cancer transplanted models,pamufetinib (200 mg/kg/d) induces a 48% regression from the initial tumor volume . ED50 of Tpamufetinib in this model is 8 mg/kg/d. Pamufetinib significantly prolongs survival of these mice when administered at doses of 50 or 200 mg/kg/d[1]. Pamufetinib inhibits angiogenesis in PC-9/HGF tumors in vivo. Moreover, the doublet erlotinib and pamufetinib successfully inhibit PC-9/HGF tumor growth and delay tumor regrowth associated with sustained tumor vasculature inhibition even after cessation of the treatment[2].

Synonyms	H2OL3Q4XRD, 4-(2-Fluoro-4-(3-(2-phenylacetyl)thioureido)phenoxy)-7-methoxy-N-methylquinoline-6-carboxamide, TAS-115
Molecular Weight	518.56
Formula	C27H23FN4O4S
CAS No.	1190836-34-0

Storage

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

Solubility Information

DMSO: 13 mg/ml (25.07 mM)

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.

Related compound libraries

This product is contained In the following compound libraries：

Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Inhibitor Library Cytokine Inhibitor Library ReFRAME Related Library Anti-Breast Cancer Compound Library Anti-Pancreatic Cancer Compound Library Bioactive Compound Library Natural Product Library for HTS Anti-Tumor Natural Product Library

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Related compounds with same targets

VEGFR-2-IN-36 ZM323881 hydrochloride Nintedanib esylate AAL-993 GW806742X JK-P3 VEGFR-2-IN-37 TAK-593

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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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Keywords

Pamufetinib 1190836-34-0 Angiogenesis Tyrosine Kinase/Adaptors VEGFR c-Met/HGFR H2OL3Q4XRD 4-(2-Fluoro-4-(3-(2-phenylacetyl)thioureido)phenoxy)-7-methoxy-N-methylquinoline-6-carboxamide Inhibitor TAS 115 inhibit TAS115 Vascular endothelial growth factor receptor TAS-115 inhibitor

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