Telaglenastat hydrochloride

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CAS NO:

1874231-60-3

CB-839 hydrochloride

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KGA和GAC，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.