Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Telaglenastat (CB-839) hydrochloride is a first-in-class, reversible, and orally active inhibitor of glutaminase 1 (GLS1). It selectively inhibits the splice variants of GLS1, specifically KGA (kidney-type glutaminase) and GAC (glutaminase C), as compared to GLS2. Telaglenastat hydrochloride has an IC50 of 23 nM for endogenous glutaminase in mouse kidney and 28 nM in the brain. In addition, it induces autophagy and exhibits antitumor activity.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 6-8周 |
Telaglenastat hydrochloride 的其他形式现货产品:
产品描述 | Telaglenastat (CB-839) hydrochloride is a first-in-class, reversible, and orally active inhibitor of glutaminase 1 (GLS1). It selectively inhibits the splice variants of GLS1, specifically KGA (kidney-type glutaminase) and GAC (glutaminase C), as compared to GLS2. Telaglenastat hydrochloride has an IC50 of 23 nM for endogenous glutaminase in mouse kidney and 28 nM in the brain. In addition, it induces autophagy and exhibits antitumor activity. |
体外活性 | Telaglenastat (CB-839) (0.1-1000 nM; 72 hours) has antiproliferative activity in HCC1806 and MDA-MB-231 cells with IC 50 s of 49 nM and 26 nM, respectively[1]. Telaglenastat (CB-839) (1 μM; 72 hours) activates caspase 3/7 and induces apoptosis in MDA-MB-231 and HCC1806 cells[1]. Cell Proliferation Assay[1]Cell Line: HCC1806, MDA-MB-231 cells Concentration: 0.1, 1, 10, 100, 1000 nM Incubation Time: 72 hours Result: Has a potent effect on the proliferation of the two TNBC cell lines (IC 50 of 49 nM and 26 nM for HCC1806 and MDA-MB-231 cells). Apoptosis Analysis[1]Cell Line: MDA-MB-231, HCC1806 cells Concentration: 1 μM Incubation Time: 72 hours Result: Caspase 3/7 activation. |
体内活性 | Telaglenastat (CB-839) (200 mg/kg; p.o.; twice daily for 28 days) has antitumor activity in xenograft models of TNBC[1]. Animal Model: Female nu/nu mice with age 4–6 weeks (TNBC patient-derived xenograft model)[1]Dosage: 200 mg/kg Administration: Oral administration; twice daily for 28 days Result: Suppressed tumor growth by 61% relative to vehicle control at the end of study. |
别名 | CB-839 hydrochloride |
分子量 | 608.04 |
分子式 | C26H25ClF3N7O3S |
CAS No. | 1874231-60-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Telaglenastat hydrochloride 1874231-60-3 CB-839 hydrochloride CB 839 Hydrochloride Telaglenastat Hydrochloride CB839 Hydrochloride CB-839 Hydrochloride Inhibitor inhibitor inhibit