IPN60090|cas:1853164-83-6|西域试剂

IPN60090,99.14%

产品编号：Bellancom-103671| CAS NO：1853164-83-6| 分子式：C₂₄H₂₇F₃N₈O₃| 分子量：532.52

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-103671	￥5800.00	杭州北京（现货）
Bellancom-103671	￥9800.00	杭州北京（现货）
Bellancom-103671	￥19000.00	杭州北京（现货）
Bellancom-103671	￥32000.00	杭州北京（现货）
Bellancom-103671	￥50000.00	杭州北京（现货）

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IPN60090

产品介绍

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。

生物活性

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.

体外研究

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 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.
IPN60090 inhibits the proliferation of A549 cells with an IC₅₀ of 26 nM.

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

体内研究

IPN60090 (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%.
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.
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. 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.

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

Animal Model:	Female CD-1 mice
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
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.

体内研究

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

Animal Model:	Female CD-1 mice
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
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.

性状

Solid

溶解性数据

In Vitro:

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

配制储备液

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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
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
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

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。