Telaglenastat hydrochloride(Synonyms: CB-839 hydrochloride)

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Telaglenastat hydrochloride (Synonyms: 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。

Telaglenastat hydrochloride(Synonyms: CB-839 hydrochloride)

Telaglenastat hydrochloride Chemical Structure

CAS No. : 1874231-60-3

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Telaglenastat hydrochloride 的其他形式现货产品:

Telaglenastat

生物活性

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

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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 (IC50 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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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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