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Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $95 | 5 days | |
5 mg | $197 | 5 days | |
50 mg | $747 | 1-2 weeks | |
100 mg | $1,240 | 1-2 weeks |
Description | TAS-115 mesylate is a potent inhibitor of VEGFR and hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase(IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively). |
Targets&IC50 | MET (rat):32 nM , VEGFR2 (rat):30 nM |
In vitro | TAS-115 powerfully suppresses the VEGF-dependent proliferation of HUVECs with IC50 of 0.019 μM as a VEGFR-targeted inhibitor and powerfully suppresses the proliferation of MET-amplified cancer cells with GI50 of 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].In PC-9 and HCC827 cells, Crizotinib and TAS-115 inhibit Met phosphorylation and reverse erlotinib resistance and VEGF production triggered by HGF [2]. |
In vivo | TAS-115 is administered daily for 6 weeks, and it can completely inhibit the progress of MET-inactivated tumors by blocking angiogenesis without toxicity, even at a serum-saturating dose of TAS-115. In MET-amplified human cancer–bearing mice, TAS-115 induces marked tumor shrinkage and prolonges survival [1]. |
Alias | TAS-115 mesylate, TAS-115 methanesulfonate |
Molecular Weight | 614.66 |
Formula | C28H27FN4O7S2 |
Cas No. | 1688673-09-7 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 75 mg/mL (122.02 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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