CB-839 (Telaglenastat) | Glutaminase-1 (GLS1) inhibitor

Chemical Structure : CB-839

CAS No.: 1439399-58-2

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CB-839 (Telaglenastat, CB839, CB 839)

货号: PC-42933Not For Human Use, Lab Use Only.

CB-839 (Telaglenastat) is a potent, selective, and orally bioavailable inhibitor of glutaminase with IC50 of 28 and 23 nM for glutaminase-1 (GLS1) in kidney and brain (GAC and KGA), but not the liver form of glutaminase (GLS2, IC50>1 uM).

规格	价格	库存
5 mg	￥780	In stock
10 mg	￥1180	In stock
50 mg	￥2580	In stock
100 mg	￥3980	In stock
250 mg		Get quote

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生物&药学活性

CB-839 (Telaglenastat) is a potent, selective, and orally bioavailable inhibitor of glutaminase with IC50 of 28 and 23 nM for glutaminase-1 (GLS1) in kidney and brain (GAC and KGA), but not the liver form of glutaminase (GLS2, IC50>1 uM).
CB-839 (Telaglenastat) demonstrates antiproliferative activity in triple-negative breast cancer (TNBC) cell line HCC-1806 and MDA-MB-231 with IC50 of 20-55 nM.
CB-839 (Telaglenastat) decreases glutamine consumption, glutamate production, oxygen consumption, and the steady-state levels of glutathione and several tricarboxylic acid cycle intermediates.
CB-839 (Telaglenastat) exhibits vivo efficacy in breast cancer xenograft models, both as a single agent and in combination with paclitaxel.

物理化学性质&存储条件

分子量	571.57
分子式	C26H24F3N7O3S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-Pyridineacetamide, N-[5-[4-[6-[[2-[3-(trifluoromethoxy)phenyl]acetyl]amino]-3-pyridazinyl]butyl]-1,3,4-thiadiazol-2-yl]-

参考文献

1. Gross MI, et al. Mol Cancer Ther. 2014 Apr;13(4):890-901.

2. Chakrabarti G, et al. Cancer Metab. 2015 Oct 12;3:12.

3. Jacque N, et al. Blood. 2015 Sep 10;126(11):1346-56.

4. Zimmermann SC, et al. ACS Med Chem Lett. 2016 Mar 13;7(5):520-4.

CB-839 (Telaglenastat, CB839, CB 839)

生物&药学活性

物理化学性质&存储条件

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CB-839 (Telaglenastat, CB839, CB 839)

生物&药学活性

物理化学性质&存储条件

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