Accueil>>Signaling Pathways>> Tyrosine Kinase>> c-MET>>TAS-115 mesylate (TAS-115 methanesulfonate)

TAS-115 mesylate (TAS-115 methanesulfonate) (Synonyms: TAS-115 mesylate)

Catalog No.GC33273

Le mésylate de pamufétinib (TAS-115) est un puissant inhibiteur de la kinase ciblant le VEGFR et le récepteur du facteur de croissance des hépatocytes (c-Met/HGFR), avec des CI50 de 30 et 32 nM pour rVEGFR2 et rMET, respectivement.

Products are for research use only. Not for human use. We do not sell to patients.

TAS-115 mesylate (TAS-115 methanesulfonate) Chemical Structure

Cas No.: 1688673-09-7

Taille Prix Stock Qté
10mM (in 1mL DMSO)
243,00 $US
En stock
5mg
180,00 $US
En stock
10mg
315,00 $US
En stock
25mg
608,00 $US
En stock
50mg
810,00 $US
En stock
100mg
1 350,00 $US
En stock

Tel:(909) 407-4943 Email: sales@glpbio.com

Avis des clients

Based on customer reviews.

  • GlpBio Citations

    GlpBio Citations
  • Bioactive Compounds Premium Provider

    Bioactive Compounds Premium Provider

Sample solution is provided at 25 µL, 10mM.

Description Protocol Chemical Properties Product Documents Related Products

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

TAS-115 powerfully suppresses the VEGF-dependent proliferation of HUVECs (IC50=0.019 μM) as a VEGFR-targeted inhibitor and powerfully suppresses the proliferation of MET-amplified cancer cells (GI50=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]. Crizotinib and TAS-115 inhibit Met phosphorylation and reverse erlotinib resistance and VEGF production triggered by HGF in PC-9 and HCC827 cells[2].

TAS-115 completely suppresses the progression of MET-inactivated tumor by blocking angiogenesis without toxicity when given every day for 6 weeks, even at a serum-saturating dose of TAS-115. TAS-115 induces marked tumor shrinkage and prolonges survival in MET-amplified human cancer-bearing mice[1].

[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.

Avis

Review for TAS-115 mesylate (TAS-115 methanesulfonate)

Average Rating: 5 ★★★★★ (Based on Reviews and 18 reference(s) in Google Scholar.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%
Review for TAS-115 mesylate (TAS-115 methanesulfonate)

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.