TAS-115 mesylate (TAS-115 methanesulfonate)

A multi-kinase inhibitor

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库存: 现货

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5mg

￥2175.00

1740.00

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10mg

￥3775.00

3020.00

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25mg

￥7287.00

5830.00

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50mg

￥9712.00

7770.00

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100mg

￥16025.00

12820.00

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Background

TAS 115 is a multi-kinase inhibitor that inhibits the growth factor receptors PDGFRα and PDGFRβ (IC₅₀s = 0.81 and 7.06 nM, respectively), c-FMS (IC₅₀ = 15 nM), VEGFR2 and VEGFR1 (IC₅₀s = 30 and 140 nM, respectively), Met (IC₅₀ = 32 nM), and FGFR2 (IC₅₀ = 340 nM).^1,2 It also inhibits Axl, c-Kit, Src, and FLT1.¹ TAS 115 inhibits VEGF-induced VEGFR2 phosphorylation in human umbilical vein endothelial cells (HUVECs) and Met phosphorylation in Met-amplified MKN45 human gastric cancer cells. It also inhibits VEGF-dependent, but not VEGF-independent, growth of HUVECs (IC₅₀s = 0.019 and 19.3 ?M, respectively) and of Met-amplified MKN45, but not Met-inactivated, human MCF-7 breast cancer cells (GI₅₀s = 0.032 and >10 ?M, respectively). TAS 115 reduces tumor growth in a MKN45 mouse xenograft model (ED₅₀ = 8 mg/kg).

1.Fujita, H., Miyadera, K., Kato, M., et al.The novel VEGF receptor/MET-targeted kinase inhibitor TAS-115 has marked in vivo antitumor properties and a favorable tolerability profileMol. Cancer Ther.12(12)2685-2696(2013) 2.Koyama, K., Goto, H., Morizumi, S., et al.The tyrosine kinase inhibitor TAS-115 attenuates bleomycin-induced lung fibrosis in miceAm. J. Respir. Cell Mol. Biol.60(4)478-487(2019)

Protocol

Cell experiment:

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 experiment:

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].

参考文献:

[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.
[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.