Telaglenastat CB-839|cas:1439399-58-2|西域试剂

Telaglenastat CB-839,99.82%

产品编号：Bellancom-12248| CAS NO：1439399-58-2| 分子式：C₂₆H₂₄F₃N₇O₃S| 分子量：571.57

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-12248	￥600.00	杭州北京（现货）
Bellancom-12248	￥900.00	杭州北京（现货）
Bellancom-12248	￥1500.00	杭州北京（现货）
Bellancom-12248	￥4500.00	杭州北京（现货）
Bellancom-12248	￥6750.00	杭州北京（现货）

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Telaglenastat CB-839

产品介绍

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。

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 inuduces autophagy and has antitumor activity.

体外研究

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.
Telaglenastat (CB-839) (1 μM; 72 hours) activates caspase 3/7 and induces apoptosis in MDA-MB-231 and HCC1806 cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

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

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.

西域 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)
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.

体内研究

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

西域 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)
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.

体内研究

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

西域 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)
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (87.48 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