產(chǎn)品屬性：
產(chǎn)品名稱 | 規(guī)格 | CAS號(hào) | 型號(hào) |
IPN60090 | 5 mg 10 mg 25 mg 50 mg 100 mg | 1853164-83-6 | EY-Y0164850 |
Cas No.1853164-83-6
別名 N/A
化學(xué)名 N/A
分子式 C24H27F3N8O3
分子量 532.52
溶解度 DMSO : 31.43 mg/mL (59.02 mM; Need ultrasonic)
儲(chǔ)存條件 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
產(chǎn)品描述：
There are two known isoforms of glutaminase: GLS-1 (also called kidney-type or KGA), and GLS-2 (also called liver-type or LGA). GLS-1 is ubiquitous and GLS-2 expression appears limited primarily to the liver.In a dual-coupled enzyme assay, IPN60090 inhibits purified recombinant human GLS-1 (GAC isoform) with an IC50 of 31 nM, and has no activity against GLS-2, with an IC50 of >50000 nM[2].IPN60090 inhibits the proliferation of A549 cells with an IC50 of 26 nM[2].
IPN60090 (3 mg/kg for i.v.; 10 mg/kg for p.o.) has excellent pharmacokinetic properties, with CL=4.1 mL/min/kg, t1/2=1 hour, Cmax=19 μM, F%=89%[2].IPN-60090 (oral administration; 100 mg/kg; twice daily; 30 days) shows similar efficacy and target engagement to CB-839 dosed orally at 250 mg/kg twice daily. And the 100 mg/kg BID dose of IPN-60090 is a tolerated dose for the following model study[2].IPN-60090 (oral administration; 100 mg/kg; twice daily; 30 days; monotherapy or in combination with TAK228 ) causes tumor growth inhibition. IPN-60090 alone demonstrates robust in vivo target engagement in a dose-dependent manner. The glutamate/glutamine ratios and the free plasma concentrations of IPN-60090 at 4 hours post-dose on both day 4 and day 28 are all decreased[2]. Furthermore, IPN-60090 in combination with TAK228 strongly causes an 85% tumor growth inhibition, IPN-60090 alone causes a 28% tumor growth inhibition in vivo[2].
[1]. Maria Emilia Di Francesco, et al. Gls1 inhibitors for treating disease. WO2016004404A2. [2]. Michael J Soth, et al. Discovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties. J Med Chem. 2020 Nov 12;63(21):12957-12977.
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關(guān)鍵字： 1853164-83-6;C24H27F3N8O3;IPN60090;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要從事免疫學(xué)、分子生物學(xué)和常規(guī)生化試劑等為一體的科研產(chǎn)品銷(xiāo)售企業(yè)，公司自成立以來(lái)，秉承""全心全意服務(wù)于科研工作者""的企業(yè)理念，立足生物科技領(lǐng)域，運(yùn)用生物技術(shù)和科研試劑，發(fā)展現(xiàn)代生物科技，為各類(lèi)大中小醫(yī)院及其它醫(yī)療機(jī)構(gòu)、高等院校、科研院所、企事業(yè)單位提供優(yōu)質(zhì)的產(chǎn)品，服務(wù)生物科技領(lǐng)域的科學(xué)研究人員。
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