TAS-115-mesylate-TAS-115-methanesulfonate-DataSheet-生命科學試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETAS-115 mesylateCat. No.: HY-12423ACAS No.: 1688673-09-7Synonyms: TAS-115 methanesulfonate分式: CHFNOS分量: 614.66作靶點: VEGFR; c-Met/HGFR作通路: Protein Tyrosine Kinase/RTK儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1

2、 month溶解性數(shù)據(jù)體外實驗 DMSO : 75 mg/mL (122.02 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.6269 mL 8.1346 mL 16.2692 mL5 mM 0.3254 mL 1.6269 mL 3.2538 mL10 mM 0.1627 mL 0.8135 mL 1.6269 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內實驗 請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍福渲魄罢埾扰渲瞥吻宓膬湟海僖来翁砑?/p>

3、助溶劑(為保證實驗結果的可靠性，體內實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.07 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.07 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www

4、.MedChemEBIOLOGICAL ACTIVITY物活性 TAS-115 mesylate種有效的 VEGFR 和肝細胞長因受體 (c-Met/HGFR) 的靶向激酶抑制劑，能夠抑制rVEGFR2 和 rMET 的活性，IC50 值分別為 30 和 32 nM。IC50 & Target IC50: 30 nM (rVEGFR2), 32 nM (rMET) 1體外研究 TAS-115 powerfully suppresses the VEGF-dependent proliferation of HUVECs (IC50=0.019 M) as aVEGFR-targeted inh

5、ibitor and powerfully suppresses the proliferation of MET-amplified cancer cells(GI50=0.032-0.362 M) as a MET-targeted inhibitor. TAS-115 has much less toxicity in various normal celllines when compared with other VEGFR-targeted kinase inhibitors 1. Crizotinib and TAS-115 inhibit Metphosphorylation

6、and reverse erlotinib resistance and VEGF production triggered by HGF in PC-9 andHCC827 cells 2.體內研究 TAS-115 completely suppresses the progression of MET-inactivated tumor by blocking angiogenesis withouttoxicity when given every day for 6 weeks, even at a serum-saturating dose of TAS-115. TAS-115 i

7、nducesmarked tumor shrinkage and prolonges survival in MET-amplified human cancerbearing mice 1.PROTOCOLCell Assay 2 Tumor cells (8000 cells/800 mL) with or without TAS-115 (1.0 M) or erlotinib (0.3 M) in the lower Transwellcollagencoated chambers are cocultured with MRC-5 (1000 cells/300 L) cells i

8、n the upper chamber for 72hours. The upper chamber is then removed. Cell viability is measured using the MTT assay 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 1Administration 1 The TAS-115 dose levels are set at 12.5, 50, and 200 mg/kg

9、/d. The dose level for sunitinib is set at 40mg/kg/d. Oral drug treatment is continued for 14 or 42 consecutive days for the chronic dosing in the SC-9xenograft model. During the treatment period, TV and body weight are measured twice per week. Theantitumor efficacy is assessed at the end of each st

10、udy period 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Fujita H, et al. The novel VEGF receptor/MET-targeted kinase inhibitor TAS-115 has marked in vivo antitumor properties and a favorabletolerability 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 cancerharboring an EGFR mutation. J Thorac Oncol. 2014 Jun;9(6):775-83.McePdfHeightCaution: Product has not been