產(chǎn)品目錄

規(guī)格	100mg 50mg 5mg 10mg
CAS	1439399-58-2
別名
化學名	2-(pyridin-2-yl)-N-(5-(4-(6-(2-(3-(trifluoromethoxy)phenyl)acetamido)pyridazin-3-yl)butyl)-1,3,4-thiadiazol-2-yl)acetamide
分子式	C26H24F3N7O3S
分子量	571.57
溶解度	≥ 28.6mg/mL in DMSO
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

Telaglenastat (CB-839) is a first-in-class, reversible and orally bioavailable glutaminase 1 (GLS1) inhibitor. Telaglenastat (CB-839) selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Antitumor activity[1].

Telaglenastat (CB-839) (0.1-1000 nM; 72 hours) has antiproliferative activity in HCC1806 and MDA-MB-231 cells with IC50s 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].

Telaglenastat (CB-839) (200 mg/kg; p.o.; twice daily for 28 days) has antitumor activity in xenograft models of TNBC[1].

References:

[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.

特別提醒：

1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

2. 為了您的安全和健康，請穿好實驗服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術有限公司

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