2. Apoptosis Autophagy
  3. Bcl-2 Family Autophagy
  4. Venetoclax

Venetoclax  (Synonyms: 维奈妥拉; ABT-199; GDC-0199; RG7601)

目录号: HY-15531 纯度: 99.95%
Data Sheet SDS COA 产品使用指南 技术支持

溶解度

动物溶解方案

Venetoclax (ABT-199; GDC-0199) 是一种高效，有选择性和口服有效的 Bcl-2 抑制剂，Ki 小于0.01 nM。Venetoclax 可以诱导自噬 (autophagy) 作用。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Venetoclax Chemical Structure

Venetoclax Chemical Structure

CAS No. : 1257044-40-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥802
In-stock
5 mg ￥600
In-stock
10 mg ￥840
In-stock
50 mg ￥1080
In-stock
100 mg ￥1400
In-stock
500 mg ￥3680
In-stock
1 g ￥5840
In-stock
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10 g   询价  

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Customer Review

Other Forms of Venetoclax:

Venetoclax 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 161 篇科研文献

WB

    Venetoclax purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 10;503(3):1214-1220.  [Abstract]

    Bcl-2 family protein expression is assessed by western blotting in CNE-2 and 5-8F cells after treatment with ABT-199 for 48 h.

    Venetoclax purchased from MCE. Usage Cited in: Cancer Cell. 2017 Oct 9;32(4):490-505.e10.  [Abstract]

    Immunoblot for BAX, BCL-2, BCL-XL, and MCL-1 from immunoprecipitates of BAX from OCI-AML3 cells treated with Venetoclax (1.25 μM), BTSA1 (1.25 μM), or in combination after 2.5 hr, and western blot detection for BAX, BCL-2, BCL-XL, and MCL-1.

    Venetoclax purchased from MCE. Usage Cited in: Nat Cell Biol. 2017 Oct;19(10):1226-1236.  [Abstract]

    ABT-199 inhibits various forms of oncogenic GLI activation.

    Venetoclax purchased from MCE. Usage Cited in: Translational Cancer Research. Vol 6, No 4. 2017.

    ABT-199 regulates p53/p21 signaling to induce G2/M phase arrest in DOHH2 cells. Representative blots of CDK1/cdc2, cyclin B1, p21 and p53 in DOHH2 cells treated with ABT-199 at 0.1 and 1 μM for 24 h. β-actin is used as the internal control.

    查看 Bcl-2 Family 亚型特异性产品:

    查看所有亚型
    Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy[1][2][3].

    IC50 & Target[1]

    Bcl-2

    0.01 nM (Ki)

    Bcl-xL

    48 nM (Ki)

    Bcl-W

    245 nM (Ki)

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    Cancer cell lines GI50
    2.6 μM
    Compound: ABT-199
    Cytotoxicity against human renal cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay
    Cytotoxicity against human renal cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay
    		[PMID: 27994761]
    Cancer cell lines GI50
    2.7 μM
    Compound: ABT-199
    Cytotoxicity against human non-small cell lung cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay
    Cytotoxicity against human non-small cell lung cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay
    		[PMID: 27994761]
    Cancer cell lines GI50
    2.77 μM
    Compound: ABT-199
    Cytotoxicity against human breast cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay
    Cytotoxicity against human breast cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay
    		[PMID: 27994761]
    Cancer cell lines GI50
    2.85 μM
    Compound: ABT-199
    Cytotoxicity against human colon cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay
    Cytotoxicity against human colon cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay
    		[PMID: 27994761]
    Cancer cell lines GI50
    3.33 μM
    Compound: ABT-199
    Cytotoxicity against human ovarian cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay
    Cytotoxicity against human ovarian cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay
    		[PMID: 27994761]
    Cancer cell lines GI50
    3.35 μM
    Compound: ABT-199
    Cytotoxicity against human CNS cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay
    Cytotoxicity against human CNS cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay
    		[PMID: 27994761]
    Cancer cell lines GI50
    3.51 μM
    Compound: ABT-199
    Cytotoxicity against human prostate cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay
    Cytotoxicity against human prostate cancer cells assessed as cell growth inhibition after 48 hrs by SRB assay
    		[PMID: 27994761]
    HEK-293T IC50
    > 20 μM
    Compound: ABT-199
    Cytotoxicity against HEK293T cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay
    Cytotoxicity against HEK293T cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay
    		[PMID: 34228434]
    HeLa IC50
    > 20 μM
    Compound: ABT-199
    Cytotoxicity against human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay
    Cytotoxicity against human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay
    		[PMID: 34228434]
    HL-60 IC50
    0.077 μM
    Compound: ABT-199
    Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay
    Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay
    		[PMID: 34228434]
    HL-60 EC50
    8.1 μM
    Compound: ABT-199
    Induction of apoptosis in human HL-60 cells measured after 48 hrs by FITC-Annexin V/PS staining based
    Induction of apoptosis in human HL-60 cells measured after 48 hrs by FITC-Annexin V/PS staining based
    		[PMID: 33197310]
    K562 EC50
    2.1 μM
    Compound: ABT199
    Cytotoxicity against human K562 cells assessed as cell survival measured after 72 hrs by MTT assay
    Cytotoxicity against human K562 cells assessed as cell survival measured after 72 hrs by MTT assay
    		[PMID: 34216984]
    KG-1 EC50
    0.85 μM
    Compound: ABT-199
    Induction of apoptosis in human KG-1 cells measured after 48 hrs by FITC-Annexin V/PS staining based
    Induction of apoptosis in human KG-1 cells measured after 48 hrs by FITC-Annexin V/PS staining based
    		[PMID: 33197310]
    Leukemia cell GI50
    2.11 μM
    Compound: ABT-199
    Cytotoxicity against human leukemia cells assessed as cell growth inhibition after 48 hrs by SRB assay
    Cytotoxicity against human leukemia cells assessed as cell growth inhibition after 48 hrs by SRB assay
    		[PMID: 27994761]
    MCF7 EC50
    1.35 μM
    Compound: ABT-199
    Induction of apoptosis in human MCF7 cells measured after 48 hrs by FITC-Annexin V/PS staining based
    Induction of apoptosis in human MCF7 cells measured after 48 hrs by FITC-Annexin V/PS staining based
    		[PMID: 33197310]
    Melanoma cell GI50
    1.75 μM
    Compound: ABT-199
    Cytotoxicity against human melanoma cells assessed as cell growth inhibition after 48 hrs by SRB assay
    Cytotoxicity against human melanoma cells assessed as cell growth inhibition after 48 hrs by SRB assay
    		[PMID: 27994761]
    OCI-AML-3 EC50
    6.8 μM
    Compound: ABT-199
    Induction of apoptosis in human OCI-AML-3 cells measured after 48 hrs by FITC-Annexin V/PS staining based
    Induction of apoptosis in human OCI-AML-3 cells measured after 48 hrs by FITC-Annexin V/PS staining based
    		[PMID: 33197310]
    RPMI-8226 IC50
    2.7 μM
    Compound: ABT-199
    Growth inhibition of human RPMI8226 cells after 72 hrs by MTT assay
    Growth inhibition of human RPMI8226 cells after 72 hrs by MTT assay
    		[PMID: 30594434]
    RS4-11 IC50
    0.0043 μM
    Compound: ABT-199
    Cytotoxicity against human RS4-11 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay
    Cytotoxicity against human RS4-11 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay
    		[PMID: 34228434]
    RS4-11 IC50
    0.006 μM
    Compound: ABT-199; 1
    Antiproliferative activity against human RS4:11 cells after 72 hrs by MTS assay
    Antiproliferative activity against human RS4:11 cells after 72 hrs by MTS assay
    		[PMID: 30278333]
    RS4-11 IC50
    0.33 μM
    Compound: ABT-199
    Cytotoxicity against human RS4:11 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human RS4:11 cells assessed as reduction in cell viability after 24 hrs by MTT assay
    		[PMID: 29453135]
    RS4-11 IC50
    1.8 nM
    Compound: 6; ABT-199
    Antiproliferative activity against human RS4-11 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human RS4-11 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    		[PMID: 34536651]
    Toledo IC50
    0.011 μM
    Compound: ABT-199; 1
    Antiproliferative activity against human Toledo cells after 72 hrs by MTS assay
    Antiproliferative activity against human Toledo cells after 72 hrs by MTS assay
    		[PMID: 30278333]
    U-266 IC50
    94 μM
    Compound: ABT-199
    Growth inhibition of human U266 cells after 72 hrs by MTT assay
    Growth inhibition of human U266 cells after 72 hrs by MTT assay
    		[PMID: 30594434]
    体外研究
    (In Vitro)

    Venetoclax (ABT-199) 有效杀死 FL5.12-BCL-2 细胞 (EC50=4 nM)，Venetoclax (ABT-199) 对 FL5.12-表现出更弱的活性 BCL-XL 细胞 (EC50=261 nM)。ABT-199 在细胞哺乳动物双杂交试验中也表现出选择性，它会破坏 BCL-2-BIM 复合物 (EC50=3 nM)，但对 BCL-XL 的效果要差得多-BCL-XS (EC50=2.2 μM) 或 MCL-1-NOXA 复合物[1]。

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

    Venetoclax 相关抗体:
    体内研究
    (In Vivo)

    在源自 RS4;11 细胞 (ALL) 的异种移植物模型中，单次口服剂量为 12.5 mg/kg 后，Venetoclax (ABT-199) 导致最大肿瘤生长抑制 (TGImax=47%) (P<0.001) 和肿瘤生长延迟 (TGD=26%) (P<0.05)[1]。
    用 Venetoclax (ABT-199) 100 mg/kg 处理 4 天已建立的异种移植 (T-ALL 细胞系 LOUCY 的小鼠异种移植模型) 肿瘤可显著降低白血病负担[2]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    NCT NumberSponsorConditionStart DatePhase
    NCT05745714Princess Maxima Center for Pediatric Oncology|Innovative Therapies For Children with Cancer Consortium|IBFM|Fight Kids Cancer
    Acute Lymphoblastic Leukemia, in Relapse|Lymphoblastic Lymphoma (Precursor B-Lymphoblastic Lymphoma+Leukaemia) Recurrent|Lymphoblastic Lymphoma (Precursor T-Lymphoblastic Lymphoma+Leukaemia) Recurrent|Lymphoblastic Lymphoma (Precursor B-Lymphoblastic Lymphoma+Leukaemia) Refractory|Lymphoblastic Lymphoma (Precursor T-Lymphoblastic Lymphoma+Leukaemia) Refractory
    		October 1, 2023Phase 1|Phase 2
    NCT03404193M.D. Anderson Cancer Center|National Cancer Institute (NCI)
    Acute Myeloid Leukemia|Acute Myeloid Leukemia Arising From Previous Myelodysplastic Syndrome|Blastic Plasmacytoid Dendritic Cell Neoplasm|Chronic Myelomonocytic Leukemia|Mixed Phenotype Acute Leukemia|Myelodysplastic Syndrome|Recurrent Acute Biphenotypic Leukemia|Recurrent Acute Myeloid Leukemia|Recurrent Blastic Plasmacytoid Dendritic Cell Neoplasm|Recurrent Chronic Myelomonocytic Leukemia|Recurrent Mixed Phenotype Acute Leukemia|Refractory Acute Myeloid Leukemia|Refractory Blastic Plasmacytoid Dendritic Cell Neoplasm|Refractory Chronic Myelomonocytic Leukemia|Refractory Mixed Phenotype Acute Leukemia
    		January 18, 2018Phase 2
    NCT02966756AbbVie
    Chronic Lymphocytic Leukemia (CLL)|Small Lymphocytic Lymphoma (SLL)
    		October 12, 2017Phase 2
    分子量

    868.44

    Formula

    C45H50ClN7O7S
    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    中文名称

    维奈妥拉
    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 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 77.5 mg/mL (89.24 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)

    Ethanol 中的溶解度 : < 1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.1515 mL 5.7575 mL 11.5149 mL
    5 mM 0.2303 mL 1.1515 mL 2.3030 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 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：

    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

    • 方案 一

      请依序添加每种溶剂： 10% Ethanol    60% Phosal 50 PG    30% PEG400

      Solubility: 20 mg/mL (23.03 mM); 悬浊液; 超声助溶

    • 方案 二

      请依序添加每种溶剂： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: 5 mg/mL (5.76 mM); 悬浊液; Need ultrasonic and warming and heat to 49°C

    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： 45% PEG300    5% Tween-80    50% Saline

      Solubility: 10 mg/mL (11.51 mM); 悬浊液; 超声助溶

    • 方案 二

      请依序添加每种溶剂： 15% Cremophor EL    85% Saline

      Solubility: 10 mg/mL (11.51 mM); 悬浊液; 超声助溶

    扫码获得
    动物溶解方案

    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
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， PEG300/PEG400，Tween 80，均可在 MCE 网站选购。
    纯度 & 产品资料

    纯度： 99.95%

    Data Sheet (643 KB) SDS (558 KB)

    COA (287 KB)HNMR (220 KB)LCMS (139 KB)元素分析报告 (210 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [1]

    RS4;11 cells are seeded at 50,000 per well in 96-well plates and treated with compounds diluted in half-log steps starting at 1 μM and ending at 0.00005 μM. All other leukemia and lymphoma cell lines are seeded at 15,000-20,000 cells per well in the appropriate medium and incubated with Venetoclax or Navitoclax for 48 h. Effects on proliferation are determined using Cell TiterGlo reagent. EC50 values are determined by nonlinear regression analysis of the concentration-response data. Mouse FL5.12-BCL-2 and FL5.12-BCL-XL cells are propagated and assessed. Bak-/- Bax-/- double knockout mouse embryonic fibroblasts are seeded into 96-well microtiter plates at 5,000 cells per well in DMEM supplemented with 10% FBS. Venetoclax (ABT-199) in the same culture medium is added in half-log dilutions starting at 5 μM. The cells are then incubated at 37°C (5% CO2) for 48 h, and the effects on proliferation are determined using Cell TiterGlo reagent[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Mice[2]
    Nonobese diabetic/severe combined immunodeficient γ (NSG) mice are injected at 6 weeks of age in the tail vein with 150 µL phosphate-buffered saline containing 5×106 luciferase-labeled LOUCY cells. At regular time points, the bioluminescence is measured using the IVIS Lumina II imaging system. At 6 weeks, the cells are engrafted and the mice are randomly divided into 2 groups (with an equal number of males and females in both groups), and the treatment is started on day 0. Mice are treated with Venetoclax (ABT-199) 100 mg/kg body weight or with vehicle via oral gavage for 4 consecutive days. At days 0, 2, and 4 the bioluminescene is measured.

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

    Venetoclax 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.1515 mL 5.7575 mL 11.5149 mL 28.7873 mL
    5 mM 0.2303 mL 1.1515 mL 2.3030 mL 5.7575 mL
    10 mM 0.1151 mL 0.5757 mL 1.1515 mL 2.8787 mL
    15 mM 0.0768 mL 0.3838 mL 0.7677 mL 1.9192 mL
    20 mM 0.0576 mL 0.2879 mL 0.5757 mL 1.4394 mL
    25 mM 0.0461 mL 0.2303 mL 0.4606 mL 1.1515 mL
    30 mM 0.0384 mL 0.1919 mL 0.3838 mL 0.9596 mL
    40 mM 0.0288 mL 0.1439 mL 0.2879 mL 0.7197 mL
    50 mM 0.0230 mL 0.1151 mL 0.2303 mL 0.5757 mL
    60 mM 0.0192 mL 0.0960 mL 0.1919 mL 0.4798 mL
    80 mM 0.0144 mL 0.0720 mL 0.1439 mL 0.3598 mL

    Keywords:

    Venetoclax1257044-40-8ABT-199 GDC-0199 RG7601维奈妥拉ABT199ABT 199GDC0199GDC 0199GDC-0199RG7601RG 7601RG-7601Bcl-2 FamilyAutophagyorallybioavailableInhibitorinhibitorinhibit

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