Pamufetinib mesylate

SKU: orb1708396

Description

Pamufetinib mesylate (TAS-115) is a dual VEGFR and c-Met inhibitor used in cancer research. It has been investigated in preclinical studies for its potential in treating solid tumors and has shown activity in both in vitro cellular assays and in vivo animal models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1688673-09-7
• MW: 614.67
• Purity: 98.91% (May vary between batches)
• Formula: C₂₈H₂₇FN₄O₇S₂
• SMILES: O=C(NC)C1=CC=2C(=NC=CC2OC3=CC=C(C=C3F)NC(=S)NC(=O)CC=4C=CC=CC4)C=C1OC.O=S(=O)(O)C
• Target: c-Met/HGFR,VEGFR
• Solubility: DMSO:60 mg/mL (97.61 mM)

Bioactivity

• Target IC50:
  VEGFR2 (rat):12 nM (Ki)|MET (rat):39 nM (Ki)
• In Vivo:
  Pamufetinib mesylate (50 mg/kg/d) was able to completely inhibit tumor growth during treatment. And in a MET-amplified human cancer transplant model, Pamufetinib mesylate (200 mg/kg/d) regressed tumor volume by 48% from the initial volume. In this model, the 50% effective dose (ED50) of Pamufetinib was estimated to be 8 mg/kg/d. Pamufetinib mesylate significantly prolonged survival in mice when administered at doses of 50 or 200 mg/kg/d. Meanwhile, Pamufetinib mesylate effectively inhibited angiogenesis in the PC-9/HGF tumor model. In addition, the combination of erlotinib and Pamufetinib mesylate successfully inhibited PC-9/HGF tumor growth and delayed tumor regeneration that was still associated with persistent vasculature inhibition even after cessation of treatment.
• In Vitro:
  Pamufetinib mesylate is an ATP antagonist with inhibition constants (Ki) of 12 nM and 39 nM for rVEGFR2 and rMET, respectively.It potently inhibits the kinase activity of VEGFR2 and MET and their signaling-dependent cellular growth, with effects comparable to other known VEGFR or MET inhibitors. In addition, Pamufetinib mesylate caused less damage to a variety of normal cells than other VEGFR inhibitors. At concentrations below 10 μM, Pamufetinib mesylate did not affect the growth of PC-9 or HCC827 cells, but was able to concentration-dependently reverse HGF-induced resistance in both cell lines when combined with erlotinib. In addition, Pamufetinib mesylate inhibits VEGF production and endothelial cell proliferation in cancer cells.

Storage & Handling

• Storage: keep away from direct sunlight,store at low temperature,keep away from moisture | store at -20°C | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

cMet, c-Met, c-Met/HGFR, cMet/HGFR, HGFR, rVEGFR2, rMET, TAS 115 Mesylate, TAS115 mesylate, TAS-115 mesylate, TAS-115 methanesulfonate, VEGFR

Compound Identifiers

PubChem CID

118130255