TAS-115 mesylate
Modify Date: 2024-01-02 19:42:46
TAS-115 mesylate structure
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Common Name | TAS-115 mesylate | ||
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| CAS Number | 1688673-09-7 | Molecular Weight | 614.66 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C28H27FN4O7S2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of TAS-115 mesylateTAS-115 mesylate is a potent vascular endothelial growth factor (VEGFR) and hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor, with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively. |
| Name | TAS-115 mesylate |
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| Description | TAS-115 mesylate is a potent vascular endothelial growth factor (VEGFR) and hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor, with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively. |
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| Related Catalog | |
| Target |
IC50: 30 nM (rVEGFR2), 32 nM (rMET)[1] |
| In Vitro | TAS-115 powerfully suppresses the VEGF-dependent proliferation of HUVECs (IC50=0.019 μM) as a VEGFR-targeted inhibitor and powerfully suppresses the proliferation of MET-amplified cancer cells (GI50=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]. Crizotinib and TAS-115 inhibit Met phosphorylation and reverse erlotinib resistance and VEGF production triggered by HGF in PC-9 and HCC827 cells[2]. |
| In Vivo | TAS-115 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 TAS-115. TAS-115 induces marked tumor shrinkage and prolonges survival in MET-amplified human cancer–bearing mice[1]. |
| Cell Assay | 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[2]. |
| Animal Admin | Mice[1] The TAS-115 dose levels are set at 12.5, 50, and 200 mg/kg/d. The dose level for sunitinib is set at 40 mg/kg/d. Oral drug treatment is continued for 14 or 42 consecutive days for the chronic dosing in the SC-9 xenograft model. During the treatment period, TV and body weight are measured twice per week. The antitumor efficacy is assessed at the end of each study period[1]. |
| References |
| Molecular Formula | C28H27FN4O7S2 |
|---|---|
| Molecular Weight | 614.66 |
| Storage condition | 2-8℃ |