2. Metabolic Enzyme/Protease Autophagy
  3. Glutaminase Autophagy
  4. Telaglenastat

Telaglenastat  (Synonyms: CB-839)

目录号: HY-12248 纯度: 99.82%
COA 产品使用指南

摩尔计算器

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。

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Telaglenastat Chemical Structure

Telaglenastat Chemical Structure

CAS No. : 1439399-58-2

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1132
In-stock
2 mg ￥600
In-stock
5 mg ￥900
In-stock
10 mg ￥1100
In-stock
50 mg ￥2900
In-stock
100 mg ￥4640
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Telaglenastat:

Telaglenastat 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 70 篇科研文献

WB
Proliferation Assay

    Telaglenastat purchased from MCE. Usage Cited in: Pathol Int. 2023 Feb 24.  [Abstract]

    Telaglenastat (1, 2.5, 5, 10 μM; 5 days) inhibits the proliferation of DeGISTL1 cells dose-dependently.

    Telaglenastat purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2019 Jun;40(6):814-822.  [Abstract]

    The protein expression levels of the genes related to cell cycle and metabolism are detected by immunoblotting using the corresponding antibodies in H1299 cells treated with 20 nM THZ1 alone or in combination with 500 nM CB-839 for 48 h.

    Telaglenastat purchased from MCE. Usage Cited in: Am J Respir Cell Mol Biol. 2018 Mar;58(3):378-390.  [Abstract]

    Human normal lung fibroblasts are treated as in A. Levels of the indicated proteins are determined by Western blotting. CB-839 remarkably inhibits the expression of Collagens I and III in myofibroblasts.

    Telaglenastat purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Oct 2;504(2):415-421.  [Abstract]

    PC3 cells are treated with indicated doses of CB-839 for 24 h after c-Myc overexpression. Cells are then harvested for the determination of indicated proteins levels.

    Telaglenastat purchased from MCE. Usage Cited in: Cancer Discov. 2017 Apr;7(4):380-390.  [Abstract]

    MEFs treated with 12.5 nM CB-839 or control (one-way ANOVA).

    Telaglenastat purchased from MCE. Usage Cited in: Blood Adv. 2017 Jul 14;1(17):1296-1305.  [Abstract]

    The drug could be detected through MS only in the plasma from rats receiving its administration, confirming its systemic bioavailability after the treatment. Labeling scheme in panels B and C is based on the presence (+) or absence (−) of shock, DMSO (control for vehicle to the drug CB-839), and glutaminase inhibitor. Three columns are graphed per each group, indicating baseline, postshock, and end-of-shock values.

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    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[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].

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

    Telaglenastat 相关抗体:

    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].

    MCE 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
    性状

    固体

    颜色

    Off-white to yellow

    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 1 year
    -20°C 6 months
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 50 mg/mL (87.48 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    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
    查看完整储备液配制表

    * 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 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。

    • 方案 一

      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); 澄清溶液; 超声助溶

    • 方案 二

      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); 悬浊液; 超声助溶 (可加热至 55°C)

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料

    纯度: 99.82%

    COA (189 KB) HNMR (240 KB) LCMS (123 KB) 元素分析报告 (205 KB)

    产品使用指南 (1538 KB)
    参考文献

    Telaglenastat 相关分类

    完整储备液配制表

    * 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7496 mL 8.7478 mL 17.4957 mL 43.7392 mL
    5 mM 0.3499 mL 1.7496 mL 3.4991 mL 8.7478 mL
    10 mM 0.1750 mL 0.8748 mL 1.7496 mL 4.3739 mL
    15 mM 0.1166 mL 0.5832 mL 1.1664 mL 2.9159 mL
    20 mM 0.0875 mL 0.4374 mL 0.8748 mL 2.1870 mL
    25 mM 0.0700 mL 0.3499 mL 0.6998 mL 1.7496 mL
    30 mM 0.0583 mL 0.2916 mL 0.5832 mL 1.4580 mL
    40 mM 0.0437 mL 0.2187 mL 0.4374 mL 1.0935 mL
    50 mM 0.0350 mL 0.1750 mL 0.3499 mL 0.8748 mL
    60 mM 0.0292 mL 0.1458 mL 0.2916 mL 0.7290 mL
    80 mM 0.0219 mL 0.1093 mL 0.2187 mL 0.5467 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Telaglenastat1439399-58-2CB-839CB839CB 839GlutaminaseAutophagyselectivetriple-negativebreastcancerTNBCantiproliferativeHCC-1806PDACcellsplicevariantsInhibitorinhibitorinhibit

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