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CAS No. : 2102101-72-2
MCE 国际站:IPN60090 dihydrochloride
产品活性: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。
研究领域:Metabolic Enzyme/Protease
作用靶点:Glutaminase
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 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.
IPN60090 dihydrochloride inhibits the proliferation of A549 cells with an IC50 of 26 nM.
In Vivo: 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%.
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.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. 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.
相关产品:Clinical Compound Library Plus | Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | Metabolism/Protease Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Orally Active Compound Library | Glutamine Metabolism Compound Library | Anti-Cancer Metabolism Compound Library | Mitochondria-Targeted Compound Library | Cuproptosis Compound Library | Heterocyclic Compound Library | Highly Selective Inhibitors Library | Glutaminase-IN-1 | ZED-1227 | Glutaminase-IN-4 | GLS1 Inhibitor-4 | Zampilimab | NC9 | Cystamine-d8 (dihydrochloride) | BJJF078 | GLS1 Inhibitor-6 | Telaglenastat | Cystamine | LWG-301 | Glutaminase C-IN-1 | IPN60090 | GK921 | JHU-083 | A-446 | 2-Amino-2-(p-tolyl)acetic acid | 6-Diazo-5-oxo-L-nor-Leucine | L-Albizziin | BPTES | GLS-1-IN-1 | NTU281 | TG-2-IN-1 | α-Glucosidase-IN-5 | UPGL00004 | GLS1 Inhibitor-3 | Glutaminase-IN-3
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