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/ Venetoclax/维奈妥拉

Venetoclax/维奈妥拉 {[allProObj[0].p_purity_real_show]}

货号：A156386 同义名： ABT-199; GDC-0199

Venetoclax (ABT-199; GDC-0199) 是一种高效、选择性且口服有效的 Bcl-2 抑制剂，Ki 小于 0.01 nM。Venetoclax 可以诱导自噬 (autophagy) 作用。ABT-199通过阻断Bcl-2与促凋亡蛋白（如Bax、Bak）的相互作用，从而释放促凋亡蛋白并激活线粒体凋亡通路。

Venetoclax/维奈妥拉 化学结构 CAS号：1257044-40-8
Venetoclax/维奈妥拉 化学结构
CAS号：1257044-40-8
Venetoclax/维奈妥拉 3D分子结构
CAS号：1257044-40-8
Venetoclax/维奈妥拉 化学结构 CAS号：1257044-40-8
Venetoclax/维奈妥拉 3D分子结构 CAS号：1257044-40-8
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Venetoclax/维奈妥拉 纯度/质量文件 产品仅供科研

货号：A156386 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >
产品名称 Bax ↓ Bcl-2 ↓ Bcl-B ↓ Bcl-w ↓ Bcl-xL ↓ Bfl-1 ↓ Mcl-1 ↓ 其他靶点 纯度
BTSA1 ✔ 99%+
HA14-1 +

Bcl-2, IC50: 9 μM

 		98%
Venetoclax ++++

Bcl-2, Ki: <0.01 nM

 		99%
Navitoclax 99%+
Obatoclax Mesylate +++

Bcl-2, Ki: 0.22 μM

 		99%
ABT-737 +++

Bcl-2, EC50: 30.3 nM

 		+

Bcl-B, EC50: 1.82 μM

 		+++

Bcl-w, EC50: 197.8 nM

 		+++

Bcl-xL, EC50: 78.7 nM

 		99%+
Gambogic Acid +

Bfl-1, IC50: 1.06 μM

Bcl-2, IC50: 1.21 μM

 		++

Bcl-B, IC50: 0.66 μM

 		++++

Bcl-w, IC50: 0.02 μM

 		+

Bcl-xL, IC50: 1.47 μM

 		+

Bfl-1, IC50: 1.06 μM

 		++

Mcl-1, IC50: 0.79 μM

 		Caspase 99% HPLC
BH3I-1 +

BH3-Bcl-xL interaction, Ki: 2.4 μM

 		99%
A-1331852 ++++

Bcl-xL, Ki: <0.01 nM

 		99%+
A-1210477 ++++

MCL-1, IC50: 26.2 nM

 		99%+
Maritoclax ✔ 97%
TW-37 +++

Bcl-2, Ki: 0.29 μM

 		+

Bcl-xL, Ki: 1.11 μM

 		+++

Mcl-1, Ki: 0.26 μM

 		98%
UMI-77 ++

Mcl-1, Ki: 490 nM

 		97%
(R)-(-)-Gossypol acetic acid ++

Bcl-2, Ki: 0.32 μM

 		++

Bcl-xL, Ki: 0.48 μM

 		+++

Mcl-1, Ki: 0.18 μM

 		99%
Sabutoclax ++

Bfl-1, IC50: 0.62 μM

Bcl-2, IC50: 0.32 μM

 		++

Bcl-xL, IC50: 0.31 μM

 		++

Bfl-1, IC50: 0.62 μM

 		+++

Mcl-1, IC50: 0.20 μM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Venetoclax/维奈妥拉 生物活性

靶点

  • Bcl-2

    Bcl-2, Ki:<0.01 nM
描述 Bcl-2 (B-cell lymphoma 2) is the first identified apoptotic regulator. It belongs to Bcl-2 family commitment to PCD, which regulates apoptosis, pro-apoptosis or anti-apoptosis. ABT-199 is a highly potent inhibitor of Bcl-2, re-engineered from ABT-263. It has subnanomolar affinity (Ki<0.010 nM, analysis by TR–FRET assay), which is over three orders of magnitude to Bcl-XL (Ki=48nM) and Bcl-W (Ki=245 nM). ABT-199 can disrupt BCL-2–BIM complex and induce multiple hallmarks of apoptosis, including cytochrome c release, caspase activation, the externalization of phosphatidylserine and the accumulation of sub-G0/G1 DNA, with lower concentration than ABT-263. Thus it facilitates ABT-199 to have cell-killing activity to Bcl-2 high-expressed NHL cell lines. ABT-199 can inhibit tumor xenograft growth as a single agent or combination with rituximab and bendamustine.[1]
作用机制 ABT-199 is complicated by the high degree of similarity within the BH3-binding domains of Bcl-2 and Bcl-XL.[1]

Venetoclax/维奈妥拉 细胞实验

Cell Line
Concentration Treated Time Description References
multiple myeloma cells 0.5 µM 48 h To evaluate the effect of Venetoclax in combination with SD6 on multiple myeloma cells, results showed that the combination significantly enhanced Venetoclax sensitivity Haematologica. 2022 Jun 1;107(6):1410-1426.
multiple myeloma cells 0.49 to 3.5 nM 48 h To evaluate the effect of Meayamycin B on the viability of multiple myeloma cells, results showed a significant decrease in cell viability Haematologica. 2022 Jun 1;107(6):1410-1426.
697 1 nM 24 h To evaluate the synergistic cytotoxicity of Venetoclax in combination with asparaginase, results showed that Venetoclax significantly enhanced the efficacy of asparaginase. Cancer Cell. 2024 Apr 8;42(4):552-567.e6.
Nalm6 1 nM 24 h To evaluate the synergistic cytotoxicity of Venetoclax in combination with asparaginase, results showed that Venetoclax significantly enhanced the efficacy of asparaginase. Cancer Cell. 2024 Apr 8;42(4):552-567.e6.
C481S BTK mutant CLL cells 5 nM 24 h To assess cell viability, Venetoclax significantly decreased cell viability, and nemtabrutinib further decreased cell viability, while ibrutinib was ineffective. J Hematol Oncol. 2022 Nov 15;15(1):166.
Primary CLL cells 5 nM 24 h To assess cell viability, Venetoclax significantly decreased cell viability, and the addition of ibrutinib or nemtabrutinib further increased cytotoxicity. J Hematol Oncol. 2022 Nov 15;15(1):166.

Venetoclax/维奈妥拉 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
NOD/SCID J mice Multiple myeloma xenograft model Venetoclax oral administration, SD6 intratumoral injection 100 mg/kg Venetoclax once daily for 15 days; SD6 once daily for 10 days To evaluate the effect of Venetoclax in combination with SD6 on multiple myeloma xenograft models, results showed that the combination significantly inhibited tumor growth and improved mouse survival Haematologica. 2022 Jun 1;107(6):1410-1426.
NSG mice B-ALL PDX models Oral 100 mg/kg Once daily for 4 weeks To evaluate the in vivo anti-leukemic effects of Venetoclax in combination with asparaginase, results showed that the combination therapy significantly reduced the peripheral blood leukemia burden and prolonged the survival of mice. Cancer Cell. 2024 Apr 8;42(4):552-567.e6.
Mice Eμ-TCL1 adoptive transfer model Oral gavage 100 mg/kg Daily, continuous treatment To assess the survival benefit of Venetoclax in combination with BTK inhibitors, the combination of Venetoclax and nemtabrutinib significantly prolonged survival in mice. J Hematol Oncol. 2022 Nov 15;15(1):166.

Venetoclax/维奈妥拉 动物研究

Dose Mice: max = 100 mg/kg[3]
Administration p.o.

Venetoclax/维奈妥拉 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03342144 - Recruiting December 31, 2020 Germany ... 展开 >> Onkologische Praxis /ID# 201545 Recruiting Stuttgart, Baden-Wuerttemberg, Germany, 70174 Medizinisches Versorgungszentrum (MVZ) /ID# 201548 Recruiting Aschaffenburg, Bayern, Germany, 63739 Studienzentrum Aschaffenburg /ID# 204125 Recruiting Aschaffenburg, Bayern, Germany, 63739 Praxis Dres. Hornberger & Kollegen /ID# 202613 Recruiting Bad Reichenhall, Bayern, Germany, 83435 Onkologie am Segelfliegerdamm /ID# 202603 Recruiting Berlin, Bayern, Germany, 12487 Onkologie Hof /ID# 201531 Recruiting Hof, Bayern, Germany, 95028 Praxis Dr. Vehling-Kaiser /ID# 202614 Recruiting Landshut, Bayern, Germany, 84028 Praxis Dres. Grüner/Hejazi/Niewenhuys /ID# 202602 Recruiting Weiden i.d.OPf., Bayern, Germany, 92637 Praxis Dr. Kreher /ID# 202604 Recruiting Bad Liebenwerda, Brandenburg, Germany, 04924 MVZ Dres. Cordes & Partner /ID# 202598 Recruiting Frankfurt am Main, Hessen, Germany, 60596 OAZ Hannover /ID# 201538 Recruiting Hanover, Niedersachsen, Germany, 30171 Onkolologische Praxis Oldenburg /ID# 202607 Recruiting Oldenburg, Niedersachsen, Germany, 26121 MVZ der Paracelsus-Klinik /ID# 201541 Recruiting Osnabrück, Niedersachsen, Germany, 49076 Med. Studiengesellschaft Nord West GmbH /ID# 201535 Recruiting Westerstede, Niedersachsen, Germany, 26655 Onkozentrum Dresden /ID# 202599 Recruiting Dresden, Sachsen, Germany, 01127 BAG Freiberg-Richter /ID# 201532 Recruiting Dresden, Sachsen, Germany, 01307 Onkologische Schwerpunktpraxis /ID# 200953 Recruiting Berlin, Germany, 10707 Internistische Schwerpunktprax /ID# 200949 Recruiting Erlangen, Germany, 91052 Luebecker Oncology Practice /ID# 200952 Recruiting Luebeck, Germany, 23562 Stauferklinikum Schwaebisch Gm /ID# 201518 Recruiting Mutlangen, Germany, 73557 收起 <<
NCT03112174 Mantle-Cell Lymphoma Phase 3 Recruiting September 2022 -
NCT03672695 Acute Myeloid Leukaemia Phase 1 Not yet recruiting March 31, 2022 United States, Connecticut ... 展开 >> Smilow Cancer Hospital at Yale Not yet recruiting New Haven, Connecticut, United States, 06511 United States, Texas The University of Texas MD Anderson Cancer Center, Houston, TX Not yet recruiting Houston, Texas, United States, 77030 Australia Peter MacCallum cancer centrer Not yet recruiting Melbourne, Australia The Alfred Hospital Department of Haematology Not yet recruiting Victoria Park, Australia France Institut Paoli-Calmettes Not yet recruiting Marseille, France Hopital Saint-Antoine Not yet recruiting Paris, France Institut Universitaire du Cancer Toulouse - Oncopole Not yet recruiting Toulouse, France 收起 <<

Venetoclax/维奈妥拉 参考文献

[1]Souers AJ, Leverson JD, et al. ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat Med. 2013 Feb;19(2):202-8.

[2]Choo EF, Boggs J, et al. The role of lymphatic transport on the systemic bioavailability of the Bcl-2 protein family inhibitors navitoclax (ABT-263) and ABT-199. Drug Metab Dispos. 2014 Feb;42(2):207-12.

[3]Punnoose EA, Leverson JD, et al. Expression Profile of BCL-2, BCL-XL, and MCL-1 Predicts Pharmacological Response to the BCL-2 Selective Antagonist Venetoclax in Multiple Myeloma Models. Mol Cancer Ther. 2016 May;15(5):1132-44.

Venetoclax/维奈妥拉 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.15mL

0.23mL

0.12mL

5.76mL

1.15mL

0.58mL

11.51mL

2.30mL

1.15mL

Venetoclax/维奈妥拉 技术信息

CAS号1257044-40-8
分子式C45H50ClN7O7S
分子量 868.44
SMILES Code O=C(NS(=O)(C1=CC=C(NCC2CCOCC2)C([N+]([O-])=O)=C1)=O)C3=CC=C(N4CCN(CC5=C(C6=CC=C(Cl)C=C6)CC(C)(C)CC5)CC4)C=C3OC7=CN=C(NC=C8)C8=C7
MDL No. MFCD23160052
别名 ABT-199; GDC-0199; RG7601
运输蓝冰
InChI Key LQBVNQSMGBZMKD-UHFFFAOYSA-N
Pubchem ID 49846579
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C
溶解方案

DMSO: 80 mg/mL(92.12 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 二
方案 三
方案 四
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在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
方案 二

Tags: Venetoclax | ABT-199;GDC-0199;RG 7601. Venetoclax.;RG7601 | Apoptosis | Bcl-2 | AmBeed-信号通路专用抑制剂 | Venetoclax/维奈妥拉 纯度/质量文件 | Venetoclax/维奈妥拉 亚型比较 | Venetoclax/维奈妥拉 生物活性 | Venetoclax/维奈妥拉 动物研究 | Venetoclax/维奈妥拉 临床数据 | Venetoclax/维奈妥拉 参考文献 | Venetoclax/维奈妥拉 实验方案 | Venetoclax/维奈妥拉 技术信息

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