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TAS-115 mesylate

Cat. No. M10511
TAS-115 mesylate Structure
Synonym:

Pamufetinib mesylate

Size Price Availability Quantity
10mg USD 350  USD350 In stock
25mg USD 650  USD650 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

TAS-115 (Pamufetinib) mesylate inhibited the kinase activity of both VEGFR2 and MET and their signal-dependent cell growth as strongly as other known VEGFR or MET inhibitors, with IC50 values of 30 and 32 nM for rVEGFR2 and rMET, respectively.

In vivo, TAS-115 (Pamufetinib) completely suppressed 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 (Pamufetinib) induced marked tumor shrinkage and prolonged survival in MET-amplified human cancer-bearing mice. TAS-115 is a unique VEGFR/MET-targeted inhibitor with improved antitumor efficacy and decreased toxicity.

Protocol
Cell Experiment
Cell lines PC-9 (del E746_A750) and HCC827
Preparation method Tumor cells (8000 cells/800 mL) with or without TAS-115 (1.0 μM) or erlotinib (0.3 μM) in the lower Transwell collagen–coated chambers are cocultured with MRC-5 (1000 cells/300 μL) cells in the upper chamber for 72 hours. The upper chamber is then removed. Cell viability is measured using the MTT assay.
Concentrations 1.0 μmol/liter
Incubation time 72 hours
Animal Experiment
Animal models SC-9 tumor-bearing nude mice
Formulation -
Dosages 12.5, 50, and 200 mg/kg/d
Administration orally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 614.66
Formula C28H27FN4O7S2
CAS Number 1688673-09-7
Purity >99%
Solubility DMSO 65 mg/mL
Storage 2-8°C, dry, sealed
References

[1] Kazuya Koyama, et al. Am J Respir Cell Mol Biol. The Tyrosine Kinase Inhibitor TAS-115 Attenuates Bleomycin-induced Lung Fibrosis in Mice

[2] Shutaro Yamada, et al. BMC Cancer. Therapeutic potential of TAS-115 via c-MET and PDGFRα signal inhibition for synovial sarcoma

[3] Junya Nakade, et al. J Thorac Oncol. Triple inhibition of EGFR, Met, and VEGF suppresses regrowth of HGF-triggered, erlotinib-resistant lung cancer harboring an EGFR mutation

[4] Hidenori Fujita, et al. Mol Cancer Ther. The novel VEGF receptor/MET-targeted kinase inhibitor TAS-115 has marked in vivo antitumor properties and a favorable tolerability profile

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: TAS-115 mesylate, Pamufetinib mesylate supplier, VEGFR/PDGFR, inhibitors

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