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

Telaglenastat  (Synonyms: CB-839)

目錄號: HY-12248 純度: 99.82%
COA 產(chǎn)品使用指南 技術(shù)支持

Telaglenastat (CB-839) 是一種首創(chuàng)的，選擇性的，可逆性的，口服活性的谷氨酰胺酶 1 (GLS1) 抑制劑。Telaglenastat 抑制 GLS1 剪接變異體 KGA 和 GAC，比 GLS2 具有更高的選擇性。Telaglenastat 對小鼠類腎和腦中的內(nèi)源性谷氨酰胺酶的 IC50 值分別為 23 nM 和 28 nM。Telaglenastat 還可誘導(dǎo)細胞自噬 (autophagy)，并具有強大的抗腫瘤活性。

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Telaglenastat Chemical Structure

Telaglenastat Chemical Structure

CAS No. : 1439399-58-2

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1132
In-stock
1 mg ￥400
In-stock
2 mg ￥600
In-stock
5 mg ￥900
In-stock
10 mg ￥1100
In-stock
25 mg ￥1840
In-stock
50 mg ￥2900
In-stock
100 mg ￥4640
In-stock
500 mg 現(xiàn)貨 詢價
1 g   詢價  
5 g   詢價  

* Please select Quantity before adding items.

Customer Review

Other Forms of Telaglenastat:

MCE 顧客使用本產(chǎn)品發(fā)表的 78 篇科研文獻

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

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    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]
    細胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    0.026 μM
    Compound: CB-839
    Antiproliferative activity against human A549 cells incubated for 72 hrs by Celltiter-Glo assay
    Antiproliferative activity against human A549 cells incubated for 72 hrs by Celltiter-Glo assay
    		[PMID: 36038117]
    A549 IC50
    0.04 μM
    Compound: CB-839
    Antiproliferative activity against human A549 cells after 5 days by EZMTT reagent-based assay
    Antiproliferative activity against human A549 cells after 5 days by EZMTT reagent-based assay
    		[PMID: 30543285]
    A549 IC50
    6 nM
    Compound: 4, CB-839
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by celltiter-fluor assay
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability measured after 72 hrs by celltiter-fluor assay
    		[PMID: 33118821]
    CAKI-1 IC50
    0.04 μM
    Compound: CB-839
    Antiproliferative activity against human Caki1 cells after 5 days by EZMTT reagent-based assay
    Antiproliferative activity against human Caki1 cells after 5 days by EZMTT reagent-based assay
    		[PMID: 30543285]
    CT26 IC50
    0.42 μM
    Compound: I-6; CB839
    Antiproliferative activity against mouse CT26 cells overexpressing GLS1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against mouse CT26 cells overexpressing GLS1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    		[PMID: 35428013]
    H22 IC50
    > 10 μM
    Compound: CB-839
    Antiproliferative activity against mouse H22 cells after 5 days by EZMTT reagent-based assay
    Antiproliferative activity against mouse H22 cells after 5 days by EZMTT reagent-based assay
    		[PMID: 30543285]
    H22 IC50
    1.34 μM
    Compound: I-6; CB839
    Antiproliferative activity against mouse H22 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against mouse H22 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    		[PMID: 35428013]
    HCC1806 IC50
    100 nM
    Compound: 71; CB-839
    Anticancer activity against human HCC1806 cells assessed as cell growth inhibition incubated for 72 hrs by CellTiter-Blue assay
    Anticancer activity against human HCC1806 cells assessed as cell growth inhibition incubated for 72 hrs by CellTiter-Blue assay
    		[PMID: 33650861]
    HCC827 IC50
    51.42 μM
    Compound: CB-839
    Cytotoxicity against human erlotinib-resistant HCC827 cells assessed as growth inhibition after 48 hrs by CCK8 assay
    Cytotoxicity against human erlotinib-resistant HCC827 cells assessed as growth inhibition after 48 hrs by CCK8 assay
    		[PMID: 28174105]
    HCT-116 IC50
    0.028 μM
    Compound: CB-839
    Antiproliferative activity against human HCT116 cells after 5 days by EZMTT reagent-based assay
    Antiproliferative activity against human HCT116 cells after 5 days by EZMTT reagent-based assay
    		[PMID: 30543285]
    HCT-116 IC50
    0.06 μM
    Compound: I-6; CB839
    Antiproliferative activity against human HCT-116 cells overexpressing GLS1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human HCT-116 cells overexpressing GLS1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    		[PMID: 35428013]
    HCT-116 IC50
    0.06 μM
    Compound: CB839
    Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 31603674]
    HCT-116 IC50
    0.11 μM
    Compound: CB839; I-4
    Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 33792311]
    HT-1080 IC50
    44.38 μM
    Compound: CB-839
    Cytotoxicity against human HT1080 cells assessed as growth inhibition after 48 hrs by CCK8 assay
    Cytotoxicity against human HT1080 cells assessed as growth inhibition after 48 hrs by CCK8 assay
    		[PMID: 28174105]
    MDA-MB-231 IC50
    33 nM
    Compound: CB-839
    Cytotoxicity against human MDA-MB-231 cells measured on 6th day by hemocytometry
    Cytotoxicity against human MDA-MB-231 cells measured on 6th day by hemocytometry
    		[PMID: 26988803]
    MDA-MB-231 IC50
    50 nM
    Compound: 71; CB-839
    Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by CellTiter-Blue assay
    Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by CellTiter-Blue assay
    		[PMID: 33650861]
    MDA-MB-436 IC50
    0.41 μM
    Compound: I-6; CB839
    Antiproliferative activity against human MDA-MB-436 cells overexpressing GLS1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-436 cells overexpressing GLS1 assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    		[PMID: 35428013]
    MDA-MB-436 IC50
    0.43 μM
    Compound: CB839; I-4
    Antiproliferative activity against human MDA-MB-436 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-436 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 33792311]
    MDA-MB-436 IC50
    0.52 μM
    Compound: CB839
    Antiproliferative activity against human MDA-MB-436 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-436 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 31603674]
    NCI-H1703 GI50
    0.008 μM
    Compound: 5; CB-839
    Antiproliferative activity against human NCI-H1703 cells assessed as reduction in cell growth after 5 days by SYTOX green staining-based assay
    Antiproliferative activity against human NCI-H1703 cells assessed as reduction in cell growth after 5 days by SYTOX green staining-based assay
    		[PMID: 31199640]
    NCI-H358 IC50
    > 1 μM
    Compound: CB-839
    Antiproliferative activity against human NCI-H358 cells incubated for 72 hrs by Celltiter-Glo assay
    Antiproliferative activity against human NCI-H358 cells incubated for 72 hrs by Celltiter-Glo assay
    		[PMID: 36038117]
    NCI-H460 IC50
    0.036 μM
    Compound: CB-839
    Antiproliferative activity against human NCI-H460 cells incubated for 72 hrs by Celltiter-Glo assay
    Antiproliferative activity against human NCI-H460 cells incubated for 72 hrs by Celltiter-Glo assay
    		[PMID: 36038117]
    體外研究
    (In Vitro)

    Telaglenastat (CB-839) (0.1-1000 nM；72 小時) 在 HCC1806 和 MDA-MB-231 細胞中具有抗增殖活性，IC50分別為 49 nM 和 26 nM[1]。
    Telaglenastat (CB-839) (1 μM；72 小時) 可激活 caspase 3/7 并誘導(dǎo) MDA-MB-231 和 HCC1806 細胞凋亡[1]。

    MCE 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.
    體內(nèi)研究
    (In Vivo)

    Telaglenastat (CB-839)（200 mg/kg；口服；每天兩次，持續(xù) 28 天）在 TNBC 異種移植模型中具有抗腫瘤活性[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 號
    性狀

    固體

    顏色

    Off-white to yellow

    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性數(shù)據(jù)
    細胞實驗： 

    DMSO 中的溶解度 : 35 mg/mL (61.23 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    配制儲備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲存時，請在1年內(nèi)使用， -20°C儲存時，請在6個月內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗：

    以下溶解方案，請直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

    • 方案 一

      請依序添加每種溶劑： 20% HP-β-CD/10 mM Citrate pH 2.0

      Solubility: 5 mg/mL (8.75 mM); 澄清溶液; 超聲助溶

    • 方案 二

      請依序添加每種溶劑： 70% PEG300    30% (20% SBE-β-CD in Saline)

      Solubility: 4 mg/mL (7.00 mM); 懸濁液; 超聲助溶 (可加熱至 55°C)

    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實驗過程有損耗，建議您多配一只動物的量
    計算結(jié)果
    工作液所需濃度 : mg/mL
    純度 & 產(chǎn)品資料

    純度: 99.82%

    參考文獻

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲存時，請在1年內(nèi)使用， -20°C儲存時，請在6個月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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
    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.

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    產(chǎn)品名稱：
    Telaglenastat
    目錄號：
    HY-12248
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