S55746 is a potent and selective inhibitor of the anti-apoptotic protein B-cell lymphoma 2 (Bcl-2), with potential pro-apoptotic and antineoplastic activities.
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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 |
+
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 |
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 |
++
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。 |
描述 | S55746 is a potent, orally active and selective BCL-2 inhibitor with a Ki of 1.3 nM and a Kd of 3.9 nM. S55746 is effective in selectively inducing cell death through inhibition of BCL-2 in a BAX/BAK-dependent manner at a concentration of 1 μM[1]. |
Animal study | S55746 is a highly potent and well-tolerated. Administered orally at doses of 20-100 mg/kg, S55746 inhibits xenograft growth in a time- and dose-dependent manner in RS4;11 and Toledo models[1]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT02603445 | Follicular Lymphoma, Mantle Ce... 展开 >>ll Lymphoma 收起 << | Phase 1 | Completed | - | United States, New York ... 展开 >> Novartis Investigative Site New York, New York, United States, 10017 United States, Texas Novartis Investigative Site Houston, Texas, United States, 77030 Austria Novartis Investigative Site Salzburg, Austria, 5020 France Novartis Investigative Site Pierre-Benite Cedex, France, 69495 Novartis Investigative Site Toulouse Cedex 9, France, 31059 Germany Novartis Investigative Site Freiburg, Germany, 79106 Novartis Investigative Site Mainz, Germany, 55131 收起 << |
NCT02920697 | Chronic Lymphocytic Leukaemia ... 展开 >>(CLL) B-Cell Non-Hodgkin Lymphoma (NHL) Multiple Myeloma (MM) 收起 << | Phase 1 | Completed | - | Australia ... 展开 >> The Alfred Hospital Malignant Haematology & Stem Cell Transplantation Services Melbourne, Australia, 3004 France Hopital Claude Huriez Lille, France CHU de Nantes Nantes, France Centre hospitalier Lyon Sud Pierre-Bénite, France Gustave Roussy Villejuif, France Germany Universitätsklinikum Carl Gustav Carus Dresden, Germany Städtisches Klinikum Schwabing Munich, Germany Universitätsklinikum Ulm Ulm, Germany Hungary National Oncology Institute Budapest, Hungary CRU Hungary Kft Miskolc, Hungary Korea, Republic of Severance Hospital Seoul, Korea, Republic of St. Mary's Hospital Seoul, Korea, Republic of Poland Warsaw Institute of Oncology Warsaw, Poland Warsaw Medical University Warsaw, Poland Singapore National Cancer Center (NCC) Singapore, Singapore National University Cancer Institute Singapore Singapore, Singapore United Kingdom University College London Hospitals London, United Kingdom Freeman Hospital Newcastle, United Kingdom 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.41mL 0.28mL 0.14mL |
7.03mL 1.41mL 0.70mL |
14.07mL 2.81mL 1.41mL |
CAS号 | 1448584-12-0 |
分子式 | C43H42N4O6 |
分子量 | 710.817 |
别名 | BCL201 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 50 mg/mL(70.34 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 |