Powder: -20°C for 3 years | In solvent: -80°C for 2 years
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).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | 5 days | $ 67.00 | |
5 mg | 5 days | $ 197.00 |
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 | rVEGFR2:30 nM , rMET:32 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]. |
Synonyms | TAS-115 methanesulfonate, TAS-115 mesylate |
Molecular Weight | 614.66 |
Formula | C28H27FN4O7S2 |
CAS No. | 1688673-09-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
DMSO: 75 mg/mL (122.02 mM), Need ultrasonic
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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