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。
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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 |
98% | |||||||||||||||||
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 |
+
Bcl-2, IC50: 1.21 μM Bfl-1, IC50: 1.06 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 |
98% | |||||||||||||||||
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 |
98% | |||||||||||||||
Sabutoclax |
++
Bcl-2, IC50: 0.32 μM Bfl-1, IC50: 0.62 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。 |
靶点 |
|
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] |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
ALL-SIL | 10 μM | Growth Inhibition Assay | 48 h | IC50=0.1803 μM | 25301704 |
CCRF-CEM | 10 μM | Growth Inhibition Assay | 48 h | IC50=1.360 μM | 24342948 |
CS-THL1 | 20 nM | Growth Inhibition Assay | 72 h | Inhibits cell growth assessed by cell viability | 25916698 |
CS-THL1 | 25 nM | Apoptotic Assay | Induces apoptosis | 25916698 | |
Dose | Mice: max = 100 mg/kg[3] |
Administration | p.o. |
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 << |
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 |
CAS号 | 1257044-40-8 |
分子式 | C45H50ClN7O7S |
分子量 | 868.44 |
别名 | ABT-199;GDC-0199;RG 7601. Venetoclax.;RG7601 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
溶解度 |
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 |
动物实验配方 |
5% DMSO+50% PEG 300+5% Tween 80+water 5 mg/mL |