Telaglenastat-CB-839-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETelaglenastatCat. No.: HY-12248CAS No.: 1439399-58-2Synonyms: CB-839分式: CHFNOS分量: 571.57作靶点: Autophagy; Glutaminase作通路: Autophagy; Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解

2、性数据体外实验 DMSO : 30 mg/mL (52.49 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (3.64 mM); Suspended solution; Need ultrasonic2. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.08 mg/mL (3.64 mM); Clear solution3. 请依序添加每种溶剂： 20% HP-CD/10

3、 mM citrate pH 2.0Solubility: 1 mg/mL (1.75 mM); Clear solution; Need ultrasonicBIOLOGICAL ACTIVITY物活性 Telaglenastat (CB-839)有效的，可服，选择性的氨酰胺酶 1 (glutaminase 1 (GLS1) 剪接变体 KGA 和GAC 的抑制剂，在肾和脑中的 IC50 值分别为 23 nM 和 28 nM。IC50 & Target IC50: 23 nM (glutaminase in kindey), 28 nM (glutaminase in brain) 1体外研究

4、 Telaglenastat (CB-839) (0.1-1000 nM; 72 hours) has antiproliferative activity in HCC1806 and MDA-MB-231cells with IC50s of 49 nM and 26 nM, respectively 1.Telaglenastat (CB-839) (1 M; 72 hours) activates caspase 3/7 and induces apoptosis in MDA-MB-231 andHCC1806 cells 1.Telaglenastat (CB-839) signi

5、ficantly improves GAC and KGA expression levels in the majority of triple-negative breast cancer (TNBC) cell lines 1.Cell Proliferation Assay 1Cell Line: HCC1806, MDA-MB-231 cellsConcentration: 0.1, 1, 10, 100, 1000 nMIncubation Time: 72 hoursResult: Has a potent effect on the proliferation of the t

6、wo TNBC cell lines (IC50 of 49 nM and 26nM for HCC1806 and MDA-MB-231 cells).Apoptosis Analysis 1Cell Line: MDA-MB-231, HCC1806 cellsConcentration: 1 MIncubation Time: 72 hoursResult: Caspase 3/7 activation.体内研究Telaglenastat (CB-839) (200 mg/kg; p.o.; twice daily for 28 days) has antitumor activity

7、in xenograft modelsof TNBC 1.Animal Model: Female nu/nu mice with age 46 weeks (TNBC patient-derived xenograft model) 1Dosage: 200 mg/kg2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEAdministration: Oral administration; twice daily for 28 daysResult: Suppressed tumor growth by 61% relative to vehi

8、cle control at the end of study.户使本产品发表的科研献 Cancer Discov. 2017 Apr;7(4):380-390. Antioxid Redox Signal. 2019 May 20;30(15):1831-1848. Cell Physiol Biochem. 2018;48(6):2318-2336. Am J Respir Cell Mol Biol. 2019 Apr 3. Am J Respir Cell Mol Biol. 2018 Mar;58(3):378-390.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Gross MI, et al. Antitumor activity of the glutaminase inhibitor CB-839 in triple-negative breast cancer. Mol Cancer Ther. 2014Apr;13(4):890-901.McePdfHeightCaution: Product has not been fully validated for medical app