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Telaglenastat hydrochloride

Telaglenastat hydrochloride

产品编号 T39309   CAS 1874231-60-3
别名: CB-839 hydrochloride

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.

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Telaglenastat hydrochloride Chemical Structure
Telaglenastat hydrochloride, CAS 1874231-60-3
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:

Telaglenastat
其他形式的 Telaglenastat hydrochloride:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: Telaglenastat hydrochloride (T39309)
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参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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TargetMol Library Books参考文献

1. Gross MI, et al. Antitumor activity of the glutaminase inhibitor CB-839 in triple-negative breast cancer. Mol Cancer Ther. 2014 Apr;13(4):890-901. 2. Biancur DE, et al. Compensatory metabolic networks in pancreatic cancers upon perturbation of glutaminemetabolism. Nat Commun. 2017 Jul 3;8:15965. 3. Zhou WJ, et al. Estrogen inhibits autophagy and promotes growth of endometrial cancer by promoting glutamine metabolism. Cell Commun Signal. 2019 Aug 20;17(1):99.

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Keywords

Telaglenastat hydrochloride 1874231-60-3 CB-839 hydrochloride CB 839 Hydrochloride Telaglenastat Hydrochloride CB839 Hydrochloride CB-839 Hydrochloride Inhibitor inhibitor inhibit

 

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