Telaglenastat(Synonyms: CB-839)

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Telaglenastat (Synonyms: CB-839) 纯度: 99.82%

Telaglenastat (CB-839) 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 抑制 GLS1 剪接变异体 KGA 和 GAC，比 GLS2 具有更高的选择性。Telaglenastat 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 还可诱导细胞自噬 (autophagy)，并具有强大的抗肿瘤活性。

Telaglenastat(Synonyms: CB-839)

Telaglenastat Chemical Structure

CAS No. : 1439399-58-2

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Telaglenastat 相关产品

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生物活性

Telaglenastat (CB-839) is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat 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 inudces autophagy and has antitumor activity[1].

IC50 & Target

IC50: 23 nM (GLS1 in kidney), 28 nM (GLS1 in brain), >1 μM (GLS2 in liver)[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].

上海金畔生物科技有限公司 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].

上海金畔生物科技有限公司 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

571.57

Formula

C26H24F3N7O3S
CAS 号

1439399-58-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 6.29 mg/mL (11.00 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7496 mL 8.7478 mL 17.4957 mL
5 mM 0.3499 mL 1.7496 mL 3.4991 mL
10 mM 0.1750 mL 0.8748 mL 1.7496 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 20% HP-β-CD/10 mM citrate pH 2.0

    Solubility: 10 mg/mL (17.50 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂： 20% SBE-β-CD/10 mM Trisodium citrate adjusted to pH 2.0 with HCL

    Solubility: 5 mg/mL (8.75 mM); Clear solution; Need ultrasonic and adjust pH to 2 with 1M HCl and heat to 55°C

  • 3.

    请依序添加每种溶剂： 70% PEG300    30% (20% SBE-β-CD in saline)

    Solubility: 4 mg/mL (7.00 mM); Suspended solution; Need ultrasonic and warming and heat to 55°C

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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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