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IPN60090 dihydrochloride

产品编号 T39544 CAS 2102101-72-2

别名: IPN60090 dihydrochloride

IPN-60090 dihydrochloride is a potent and specific inhibitor of glutaminase 1 (GLS1) with a remarkable inhibition constant (IC50) of 31 nM. It does not exhibit any inhibitory activity against GLS-2. Furthermore, IPN-60090 dihydrochloride possesses outstanding physicochemical properties and pharmacokinetic characteristics in vivo. Therefore, it is a valuable compound for researching solid tumors, including lung and ovarian cancers.

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IPN60090 dihydrochloride Chemical Structure

IPN60090 dihydrochloride, CAS 2102101-72-2

规格	价格/CNY	货期
2 mg	￥ 2,890	5日内发货
5 mg	￥ 4,820	5日内发货
25 mg	￥ 19,800	6-8周
50 mg	￥ 26,600	6-8周
100 mg	￥ 41,600	6-8周

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IPN60090 dihydrochloride 的其他形式现货产品:

IPN60090

其他形式的 IPN60090 dihydrochloride:

IPN60090
现货

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	IPN-60090 dihydrochloride is a potent and specific inhibitor of glutaminase 1 (GLS1) with a remarkable inhibition constant (IC50) of 31 nM. It does not exhibit any inhibitory activity against GLS-2. Furthermore, IPN-60090 dihydrochloride possesses outstanding physicochemical properties and pharmacokinetic characteristics in vivo. Therefore, it is a valuable compound for researching solid tumors, including lung and ovarian cancers.
靶点活性	GLS1:31 nM (IC50)
体外活性	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 IC 50 of 31 nM, and has no activity against GLS-2, with an IC 50 of >50000 nM[2]. IPN60090 dihydrochloride inhibits the proliferation of A549 cells with an IC 50 of 26 nM[2].
体内活性	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, t 1/2 =1 hour, C max =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 (HY-12248) 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 (HY-13328)) 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]. Animal Model: Female CD-1 mice[2]Dosage: 3 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis) Administration: Intravenous injection and oral administration Result: CL (4.1 mL/min/kg), t 1/2 (1 hour) for i.v.; C max (19 μM), F% (89%) for p.o.. Animal Model: Ru337 non-small cell lung cancer patient-derived xenograft (PDX) subcutaneous mouse model as monotherapy or in combination[2]Dosage: 100 mg/kg Administration: Oral administration; 100 mg/kg; twice daily; 30 days; monotherapy or in combination with TAK228 Result: Exhibited an improvement in the combination regimen group over either single agent.

别名	IPN60090 dihydrochloride
分子量	605.44
分子式	C24H29Cl2F3N8O3
CAS No.	2102101-72-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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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.

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请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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