IPN60090

Additional information:
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.|Product information|CAS Number: 1853164-83-6|Molecular Weight: 532.{{5-Ethynyl-2′-deoxyuridine} site|{5-Ethynyl-2′-deoxyuridine} PROTAC|{5-Ethynyl-2′-deoxyuridine} Purity & Documentation|{5-Ethynyl-2′-deoxyuridine} Formula|{5-Ethynyl-2′-deoxyuridine} supplier|{5-Ethynyl-2′-deoxyuridine} Autophagy} 52|Formula: C24H27F3N8O3|Chemical Name: 1-[(2R)-4-(6-{2-[4-(3,3-difluorocyclobutoxy)-6-methylpyridin-2-yl]acetamido}pyridazin-3-yl)-2-fluorobutyl]-N-methyl-1H-1,2,3-triazole-4-carboxamide|Smiles: CC1=CC(=CC(CC(=O)NC2=CC=C(CC[C@@H](F)CN3C=C(N=N3)C(=O)NC)N=N2)=N1)OC1CC(F)(F)C1|InChiKey: GEHZIZWHNLQFAS-OAHLLOKOSA-N|InChi: InChI=1S/C24H27F3N8O3/c1-14-7-18(38-19-10-24(26,27)11-19)8-17(29-14)9-22(36)30-21-6-5-16(31-33-21)4-3-15(25)12-35-13-20(32-34-35)23(37)28-2/h5-8,13,15,19H,3-4,9-12H2,1-2H3,(H,28,37)(H,30,33,36)/t15-/m1/s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 31.{{Triamcinolone acetonide} MedChemExpress|{Triamcinolone acetonide} FGFR|{Triamcinolone acetonide} Technical Information|{Triamcinolone acetonide} In Vitro|{Triamcinolone acetonide} manufacturer|{Triamcinolone acetonide} Epigenetics} 43 mg/mL (59.02 mM; Need ultrasonic).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|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.PMID:27102143 IPN60090 inhibits the proliferation of A549 cells with an IC50 of 26 nM.|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%. 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.|Products are for research use only. Not for human use.|