TAS-115 Methanesulfonic acid salt
TAS-115 Methanesulfonic acid salt Basic information
- Product Name:
- TAS-115 Methanesulfonic acid salt
- Synonyms:
-
- TAS-115 Methanesulfonic acid salt
- TAS-115 mesylate (Synonyms: TAS-115 methanesulfonate)
- TAS115;TAS 115
- TAS-115 mesylate
- TAS-115 methanesulfonate
- TAS-115 mesylate (TAS-115 methanesulfonate)
- Pamufetinib (mesylate)
- Pamufetinib (TAS-115) mesylate
- CAS:
- 1688673-09-7
- MF:
- C28H27FN4O7S2
- MW:
- 614.66
- Mol File:
- 1688673-09-7.mol
TAS-115 Methanesulfonic acid salt Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMSO: slightly soluble; PBS (pH 7.2): slightly soluble; Water: slightly soluble
- form
- A crystalline solid
- color
- White to off-white
TAS-115 Methanesulfonic acid salt Usage And Synthesis
Uses
Pamufetinib (TAS-115) mesylate is a potent VEGFRand hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor, with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.
in vivo
Pamufetinib mesylate 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 Pamufetinib mesylate. Pamufetinib mesylate induces marked tumor shrinkage and prolonges survival in MET-amplified human cancer–bearing mice[1].
References
[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. DOI:10.1158/1535-7163.MCT-13-0459
[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. DOI:10.1097/JTO.0000000000000170
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