Pamufetinib

SKU: orb1309024

Description

Pamufetinib (TAS-115) is a dual kinase inhibitor targeting VEGFR2 and c-Met with high potency, exhibiting IC50 values of 30 nM and 32 nM, respectively. It is utilized in preclinical cancer research, including studies on angiogenesis and tumor growth in both cellular and animal models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1190836-34-0
• MW: 518.56
• Purity: 99.39% (May vary between batches)
• Formula: C₂₇H₂₃FN₄O₄S
• SMILES: O(C=1C2=C(C=C(OC)C(C(NC)=O)=C2)N=CC1)C3=C(F)C=C(NC(NC(CC4=CC=CC=C4)=O)=S)C=C3
• Target: c-Met/HGFR,VEGFR
• Solubility: DMSO:13 mg/mL (25.07 mM)

Bioactivity

• Target IC50:
  c-Met:32 nM|VEGFR2:30 nM
• 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. 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.
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• 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. 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TAS115, TAS-115, TAS 115, Vascular endothelial growth factor receptor, VEGFR, VEGFR2, c-Met/HGFR, cMet, c-Met, cMet/HGFR, 4-(2-Fluoro-4-(3-(2-phenylacetyl)thioureido)phenoxy)-7-methoxy-N-methylquinoline-6-carboxamide, Pamufetinib, inhibit, H2OL3Q4XRD, Inhibitor, HGFR

Compound Identifiers

PubChem CID

44247727