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抑制剂/激动剂
囊泡 肿瘤
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Bcl-2
/ MIK665

MIK665 {[allProObj[0].p_purity_real_show]}

货号：A169993 同义名： S-64315

MIK665 is an inhibitor of induced myeloid leukemia cell differentiation protein (Mcl-1; Bcl2-L-3), with potential pro-apoptotic and antineoplastic activities.

MIK665 化学结构 CAS号：1799631-75-6
MIK665 化学结构
CAS号：1799631-75-6
MIK665 3D分子结构
CAS号：1799631-75-6
MIK665 化学结构 CAS号：1799631-75-6
MIK665 3D分子结构 CAS号：1799631-75-6
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MIK665 纯度/质量文件 产品仅供科研

货号：A169993 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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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。

MIK665 生物活性

描述 BCL-2 is the founding member of the BCL-2 family of apoptosis regulatory proteins that either induce (pro-apoptotic) or inhibit (anti-apoptotic) apoptosis. The anti-apoptotic BCL-2 is classified as an oncogene, as damage to the BCL-2 gene has been shown to cause a number of cancers, including lymphoma[1]. Myeloid cell leukemia-1 (MCL-1), a member of antiapoptotic BCL-2 family proteins, is a key regulator of mitochondrial homeostasis. Frequent overexpression of MCL-1 in human primary and drug-resistant cancer cells makes it an attractive cancer therapeutic target[2]. MIK665 is a special Mcl-1 inhibitor. It has an IC50 of 1.81 nM. In vitro, the combined inhibition of MCL1 and BCLXL resulted in significantly effective cell killing compared to single-agent treatment (p < 0.05) in multiple assays, including sphere assays. The combination-induced cell death was independent of BIM, and NOXA. Recapitulated in mouse xenograft model, the combination inhibited tumor growth, reduced sphere-forming capacity and had tolerable toxicity[3].

MIK665 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
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 <<
NCT02979366 Acute Myeloid Leukaemia (AML) ... 展开 >> Myelodysplastic Syndrome (MDS) 收起 << Phase 1 Recruiting October 2020 United States, Connecticut ... 展开 >> Patient Care Location: Smilow Cancer Hospital at Yale Recruiting New Haven, Connecticut, United States, 06511 United States, Texas The University of Texas MD Anderson Cancer Center, Department of Leukemia, Division of Cancer Medicine Recruiting Houston, Texas, United States, 77030 Australia The Alfred Hospital Department of Haematology Recruiting Melbourne, Australia, 3004 Royal Melbourne Hospital, Department of Clinical Haematology and BMT Service Recruiting Melbourne, Australia, 3050 France Institut Paoli-Calmettes Departement d'Hématologie Recruiting Marseille, France, 13009 Hôpital Saint-Antoine Département d'Hematologie Clinique et de Thérapie cellulaire Recruiting Paris, France, 75012 Spain Hospital Universitario Vall d' Hebron/VHIO Hematology Department Recruiting Barcelona, Spain, 08035 Hospital Universitario La Fe Hematology Department Recruiting Valencia, Spain, 46026 收起 <<
NCT02992483 Multiple Myeloma (MM), Lymphom... 展开 >>a, Large B-Cell, Diffuse (DLBCL), Lymphoma 收起 << Phase 1 Recruiting April 15, 2020 United States, Ohio ... 展开 >> Novartis Investigative Site Recruiting Columbus, Ohio, United States, 43210 United States, Texas Novartis Investigative Site Recruiting Houston, Texas, United States, 77030 Australia, Victoria Novartis Investigative Site Recruiting Heidelberg, Victoria, Australia, 3084 France Novartis Investigative Site Recruiting Nantes Cedex 1, France, 44093 Germany Novartis Investigative Site Recruiting Heidelberg, Germany, 69120 Novartis Investigative Site Recruiting Kiel, Germany, 24105 Italy Novartis Investigative Site Recruiting Rozzano, MI, Italy, 20089 Japan Novartis Investigative Site Recruiting Fukuoka-city, Fukuoka, Japan, 811-1395 Spain Novartis Investigative Site Recruiting Salamanca, Castilla Y Leon, Spain, 37007 收起 <<

MIK665 参考文献

[1]Abdul Shukkur Ebrahim,et al. Hematologic malignancies: newer strategies to counter the BCL-2 protein. J Cancer Res Clin Oncol. 2016. 142(9), 2013-22.

[2]Weiguo Xiang,et al. MCL-1 inhibition in cancer treatment. Onco Targets Ther. 2018. 11, 7301-7314.

[3]Nabanita Mukherjee,et al. MCL1 inhibitors S63845/MIK665 plus Navitoclax synergistically kill difficult-to-treat melanoma cells. Cell Death Dis. 2020. 11(6), 443.

MIK665 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.14mL

0.23mL

0.11mL

5.71mL

1.14mL

0.57mL

11.42mL

2.28mL

1.14mL

MIK665 技术信息

CAS号1799631-75-6
分子式C47H44ClFN6O6S
分子量 875.405
别名 S-64315
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,Store in freezer, under -20°C
溶解度

DMSO: 120 mg/mL(137.08 mM)，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

Tags: MIK665 | 1799631-75-6 | S-64315 | MIK 665 | MIK-665 | S64315 | S 64315 | MCL1 Inhibitor | Apoptosis | Bcl-2 Family | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | MIK665 纯度/质量文件 | MIK665 亚型比较 | MIK665 生物活性 | MIK665 临床数据 | MIK665 参考文献 | MIK665 实验方案 | MIK665 技术信息

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