RET Kinase Inhibitor 1CS-01Y70087_上海莼试生物技术有限公司

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一、概述：

化学性质：

规格	1mg 5mg 10mg 25mg
CAS	1627856-64-7
别名	N/A
化学名	4-(4-ethoxy-1,6-dihydro-6-oxo-3-pyridinyl)-2-fluoro-N-[5-(2,2,2-trifluoro-1,1-dimethylethyl)-3-isoxazolyl]-benzeneacetamide
分子式	C22H21F4N3O4
分子量	467.4
溶解度	DMSO : 100 mg/mL (216.57 mM);H2O : < 0.1 mg/mL (insoluble)
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

产品描述：

GSK3179106 is a potent and selective RET kinase inhibitor with an IC50 of 0.4 nM[1].

GSK3179106 (10 nM-100 μM; 8 days for TT cells, 3 days for SK-N-AS and A549 cells) inhibits the proliferation of the RET-dependent TT cell line with a mean IC50 value of 25.5 nM however has no effect on the proliferation of the RET-independent SK-NAS and A549 cell lines (mean IC50>10 μM and IC30>17 μM, respectively)[1].GSK3179106 inhibits RET phosphorylation in SK-N-AS cells and TT cells with mean IC50s of 4.6 nM and 11.1 nM, respectively[1].

GSK3179106 (3 or 10 mg/kg; orally; for 3.5 days BID) reduces the visceromotor response (VMR) in comparison to rats given an acetic acid enema and dosed with vehicle[1].

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标签：RET Kinase Inhibitor 1

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