货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
V57530-1ml	10mM in DMSO	￥4050.00 V57530-1ml ￥4050.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

V57530-1ml

10mM in DMSO

￥4050.00

货期：3-5天

产品描述：

IPN-60090 dihydrochloride 是一种具有口服活性和高选择性的谷氨酰胺酶 1 GLS1 的抑制剂 (IC50=31 nM)，对 GLS-2 无活性。IPN-60090 dihydrochloride 在体内表现出优良的物理化学和药代动力学特性。IPN-60090 dihydrochloride 可用于实体肿瘤的研究，如肺癌和卵巢癌。

体外研究：

IPN60090 dihydrochloride (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 dihydrochloride (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 dihydrochloride (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 dihydrochloride in combination with TAK228 strongly causes an 85% tumor growth inhibition, IPN-60090 alone causes a 28% tumor growth inhibition in vivo[2].

体内研究：

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 dihydrochloride 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 dihydrochloride inhibits the proliferation of A549 cells with an IC50 of 26 nM[2].

参考文献：

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.

保存条件：

-80°C 12个月; -20°C 6个月,干燥, 避光

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.652 ml	8.258 ml	16.517 ml
5 mM	0.33 ml	1.652 ml	3.303 ml
10 mM	0.165 ml	0.826 ml	1.652 ml
50 mM	0.033 ml	0.165 ml	0.33 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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