规格

价格

库存

数量

2 mg

¥ 312

现货

5 mg

¥ 509

现货

10 mg

¥ 787

现货

25 mg

¥ 1,510

现货

50 mg

¥ 2,360

现货

100 mg

¥ 3,730

现货

1 mL x 10 mM (in DMSO)

¥ 626

现货

生物活性

产品描述	Telaglenastat (CB 839) is a glutaminase 1 (GLS1) inhibitor with selective, reversible, and oral activity. Telaglenastat has antitumor activity and induces cellular autophagy.
靶点活性	MDA-MB-436 cells:0.52 μM, NCI-H4 cells:0.036 μM, CAKI-1 cells:0.04 μM, H22 cells:> 10 μM, HT1080 cells:44.38 μM, endogenous glutaminase (mouse brain):28 nM, endogenous glutaminase (mouse kidney):23 nM, TNBC:20-55 nM, A549 cells:0.026 μM, CT-26 cells:0.42 μM, HCC1806 cells:100 nM, HCC827 cells:51.42 μM, HCT116 cells:0.028 μM, NCI-H358 cells:> 1 μM, Glutaminase:24 nM
体外活性	方法：TNBC 细胞系 HCC1806、MDA-MB-231 和 ER+/HER2- 细胞系 T47D 用 Telaglenastat (0-1000 nmol/L) 处理 72 h，使用 Cell Titer Glo Assay 检测细胞活力。结果：Telaglenastat 处理对两种 TNBC 细胞系的增殖具有有效作用，IC50 为 20-55 nmol/L，但对 T47D 细胞的生存能力没有影响。[1] 方法：6种 ccRCC 细胞系 TUHR10TKB、A-704、786-O、Caki-1、A498、769-P 用 Telaglenastat (1 µM) 处理 1 h，使用 Western Blot 检测靶点蛋白表达水平。结果：在 Telaglenastat 存在下孵育细胞导致 S6 和 4E-BP1 的磷酸化降低。Telaglenastat 可能通过剥夺细胞由 GLS 分解谷氨酰胺产生的代谢产物来间接抑制 mTOR 信号传导。[2]
体内活性	方法：为检测体内抗肿瘤活性，将 Telaglenastat (200 mg/kg，25% (w/v) HPBCD in 10 mmol/L citrate, pH 2) 口服给药给携带 TNBC 患者衍生的异种移植物的 nu/nu 小鼠，每天两次，持续 28 天。结果：Telaglenastat 在 TNBC 异种移植模型中具有抗肿瘤活性。在研究结束时，相对于载体对照，Telaglenastat 抑制了 61% 的肿瘤生长。[1]
激酶实验	Inhibition of CB-839 on rHu-GAC: The enzymatic activity is measured in assay buffer containing 50 mM Tris-Acetate pH 8.6, 150 mM K2HPO4 , 0.25 mM EDTA, 0.1 mg/mL bovine serum albumin, 1 mM DTT, 2 mM NADP+ and 0.01% Triton X-100. To measure inhibition, the inhibitor (prepared in DMSO) is first pre-mixed with glutamine and glutamate dehydrogenase (GDH) and reactions are initiated by the addition of rHu-GAC. Final reactions contains 2 nM rHu-GAC, 10 mM glutamine, 6 units/mL GDH and 2% DMSO. Generation of NADPH is monitored by fluorescence (Ex340/Em460 nm) every minute for 15 minutes on a SpectraMax M5e plate reader. Relative fluorescence units (RFU) are converted to units of NADPH concentration (μM) using a standard curve of NADPH. Each assay plate incorporates control reactions that monitores the conversion of glutamate (1 to 75 μM) plus NADP+ to α-ketoglutarate plus NADPH by GDH. Under these assay conditions, up to 75 μM glutamate is stoichiometrically converts to α-ketoglutarate/NADPH by GDH. Initial reaction velocities are calculated by fitting the first 5 minutes of each progress curve to a straight line. Inhibition curves are fitted to a four-parameter dose response equation of the form: % activity = Bottom + (Top-Bottom)/(1+10^((LogIC50-X)*HillSlope)).
细胞实验	For viability assays, all cell lines are treated with CB-839 at the indicated concentrations for 72 hours and analyzed for antiproliferative effects using Cell Titer Glo.(Only for Reference)
别名	CB-839, CB839, CB 839

化学信息

分子量	571.57
分子式	C₂₆H₂₄F₃N₇O₃S
CAS No.	1439399-58-2
Smiles	FC(F)(F)Oc1cccc(CC(=O)Nc2ccc(CCCCc3nnc(NC(=O)Cc4ccccn4)s3)nn2)c1
密度	1.430 g/cm3 (Predicted)

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

实际储存温度请以COA为准

溶解度信息

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 121.3 mg/mL (212.22 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 9.3 mg/mL (16.27 mM), Suspension.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.7496 mL	8.7478 mL	17.4957 mL	87.4783 mL
5 mM	0.3499 mL	1.7496 mL	3.4991 mL	17.4957 mL
10 mM	0.1750 mL	0.8748 mL	1.7496 mL	8.7478 mL
20 mM	0.0875 mL	0.4374 mL	0.8748 mL	4.3739 mL
50 mM	0.0350 mL	0.1750 mL	0.3499 mL	1.7496 mL
100 mM	0.0175 mL	0.0875 mL	0.1750 mL	0.8748 mL

该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。

Telaglenastat

Telaglenastat

产品介绍

计算器

体内实验配液计算器

剂量转换

引用文献

关键词

Telaglenastat

Telaglenastat

Telaglenastat 相关产品

产品介绍

计算器

体内实验配液计算器

剂量转换

引用文献

关键词