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Telaglenastat hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Telaglenastat hydrochloride图片
CAS NO:1874231-60-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
CB-839 hydrochloride
产品介绍
Telaglenastat (CB-839) hydrochloride 是一种首创的,选择性的,可逆性的,口服活性的谷氨酰胺酶 1 (GLS1) 抑制剂。Telaglenastat hydrochloride 抑制GLS1剪接变异体KGAGAC,比 GLS2 具有更高的选择性。Telaglenastat hydrochloride 对小鼠类肾和脑中的内源性谷氨酰胺酶的IC50值分别为 23 nM 和 28 nM。Telaglenastat hydrochloride 还可诱导细胞自噬 (autophagy),并具有强大的抗肿瘤活性。
生物活性

Telaglenastat (CB-839) hydrochloride is a first-in-class, selective, reversible and orally activeglutaminase1 (GLS1)inhibitor. Telaglenastat hydrochloride selectively inhibitsGLS1splice variantsKGA (kidney-type glutaminase)andGAC (glutaminase C)compared to GLS2. TheIC50s are 23 nM and 28 nM for endogenousglutaminasein mouse kidney and brain, respectively. Telaglenastat hydrochloride inudcesautophagyand has antitumor activity[1].

体外研究
(In Vitro)

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].

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 (IC50of 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.
体内研究
(In Vivo)

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.
Clinical Trial
分子量

608.04

Formula

C26H25ClF3N7O3S

CAS 号

1874231-60-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.