1. Metabolic Enzyme/Protease
  2. Glutaminase
  3. IPN60090


目录号: HY-103671 纯度: 99.14%

IPN-60090 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 在体内表现出优良的物理化学和药代动力学特性。IPN-60090 可用于实体肿瘤的研究,如肺癌和卵巢癌。

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IPN60090 Chemical Structure

IPN60090 Chemical Structure

CAS No. : 1853164-83-6

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规格 价格 是否有货 数量
5 mg ¥5800
10 mg ¥9800
25 mg ¥19000
50 mg ¥32000
100 mg ¥50000
200 mg   询价  
500 mg   询价  

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IPN-60090 is an orally active and highly selective inhibitor of glutaminase 1 (GLS1; IC50=31 nM), with no activity observed against GLS-2. IPN-60090 exhibits excellent physicochemical and pharmacokinetic properties in vivo. IPN-60090 can be used for solid tumors research, such as lung and ovarian cancers[1][2].

IC50 & Target

IC50: 31 nM (GLS1)[2]

(In Vitro)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

(In Vivo)

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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), t1/2 (1 hour) for i.v.; Cmax (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.
Clinical Trial





Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
In Vitro: 

DMSO : 31.43 mg/mL (59.02 mM; Need ultrasonic)

浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8779 mL 9.3893 mL 18.7786 mL
5 mM 0.3756 mL 1.8779 mL 3.7557 mL
10 mM 0.1878 mL 0.9389 mL 1.8779 mL

储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 3.14 mg/mL (5.90 mM); Clear solution

    此方案可获得 ≥ 3.14 mg/mL (5.90 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 31.4 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。

纯度: 99.14%

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2


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