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囊泡 肿瘤
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Bcl-2 自噬
/ Obatoclax

奥巴克拉 (GX15-070) /Obatoclax {[allProObj[0].p_purity_real_show]}

货号：A272644 同义名： GX15-070

Obatoclax, a Bcl-2 homology domain-3 mimetic, antagonize all antiapoptotic Bcl-2 family proteins (average IC50, 3 μMol/L), including Mcl-1 (IC50, 2.9 μMol/L) and Bfl-1 (IC50, 5 μMol/L).

Obatoclax 化学结构 CAS号：803712-67-6
Obatoclax 化学结构
CAS号：803712-67-6
Obatoclax 3D分子结构
CAS号：803712-67-6
Obatoclax 化学结构 CAS号：803712-67-6
Obatoclax 3D分子结构 CAS号：803712-67-6
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Obatoclax 纯度/质量文件 产品仅供科研

货号：A272644 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。
产品名称 Autophagy ↓ 其他靶点 纯度
SBI-0206965 +++

ULK2, IC50: 711 nM

ULK1, IC50: 108 nM

 		97%
Hydroxychloroquine sulfate ✔ 99%
Valproic acid sodium ✔ HDAC 97%
PFK-015 ++

PFKFB3, IC50: 207 nM

 		99%+
MRT68921 hydrochloride ++++

ULK2, IC50: 1.1 nM

ULK1, IC50: 2.9 nM

 		99%+
ROC-325 ✔ 99%+
Autophinib +++

Autophagy, IC50: 40 nM

 		97%
Lys05 ✔ 99%+
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。

Obatoclax 生物活性

描述 The B-cell lymphoma 2 (Bcl-2) family of proteins is composed of both antiapoptotic members, such as Bcl-2, Bcl-xL as well as Bcl-w, and proapoptotic members. Up-regulation of the pro-survival Bcl-2 family proteins is one of the primary means for cancer cells to evade apoptosis. Obatoclax is the BCL-2 family inhibitor with Ki value ranging in 1-7μM (measured by FP assays) for all the six members, BCL-2, BCL-XL, MCL-1, BCL-w, A1 and BCL-b of their cytosolic domains. The in vitro study showed that obatoclax at concentration of 10-500nM can potently inhibit the association of MCL-1 and BAK extracted from SK-Mel5 cells or in intact mitochondria. Obatoclax can induce apoptosis and inhibit colony formation in cells dependent of BAX or BAK. Treatment with 0.1μM obatoclax overcame MCL-1-mediated resistance to ABT-737, leading to cell death in combination, as well as caused a modest increase of BID, NOXA, BIM and PUMA, the BH3-only members reported to antagonize MCL-1 in KB/BCL-2 cells over-expressing BCL-2. Also obatoclax can overcome MCL-1-mediated resistance to bortezomib. Treatment with obatoclax at concentration of 50 or 500nM for 24h significantly increased the apoptosis in mouse melanoma B16-F1 cells. These suggested that obatoclax may be the potential compound used to treatment where MCL-1 contributes to resistance to cell killing[1]. Obatoclax at dose of 3mg/kg markedly potentiated carfilzomib-induced-tumor growth suppression in an in vivo SUDHL4 xenograft model[2].
作用机制 Obatoclax can occupy a hydrophobic pocket within the BH3 binding groove of BCL-2 and thus interferes with MCL-1/BAK interactions.[1]

Obatoclax 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
22RV1 Growth Inhibition Assay IC50=0.27378 μM SANGER
23132-87 Growth Inhibition Assay IC50=0.82843 μM SANGER
5637 Growth Inhibition Assay IC50=0.08367 μM SANGER
639-V Growth Inhibition Assay IC50=0.15596 μM SANGER

Obatoclax 动物研究

Dose Nude Mice: 1.25 mg/kg - 5 mg/kg[3] (i.v.)
Administration i.v.

Obatoclax 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
NCT01150656 - Completed - -
NCT00438178 Hematological Malignancies Phase 1 Completed - United States, District of Col... 展开 >>umbia Georgetown University Medical Center Washington, District of Columbia, United States, 20007 United States, Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 Canada, Ontario Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 收起 <<
NCT00360035 Myelofibrosis Phase 2 Completed - United States, District of Col... 展开 >>umbia Georgetown University Medical Center Washington, District of Columbia, United States, 20007 United States, Florida James A. Haley Veterans Hospital Tampa, Florida, United States, 33612 United States, Georgia Emory University Atlanta, Georgia, United States, 30322 United States, Illinois The University of Chicago Chicago, Illinois, United States, 60637 United States, Massachusetts University of Massachusetts Medical Center Worcester, Massachusetts, United States, 01655 United States, Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 Canada, Ontario Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 收起 <<

Obatoclax 参考文献

[1]Nguyen M, Marcellus RC, et al. Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis. Proc Natl Acad Sci U S A. 2007 Dec 4;104(49):19512-7. Epub 2007 Nov 26.

[2]Dasmahapatra G, Lembersky D, et al. Obatoclax interacts synergistically with the irreversible proteasome inhibitor carfilzomib in GC- and ABC-DLBCL cells in vitro and in vivo. Mol Cancer Ther. 2012 May;11(5):1122-32.

Obatoclax 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.15mL

0.63mL

0.32mL

15.75mL

3.15mL

1.58mL

31.51mL

6.30mL

3.15mL

Obatoclax 技术信息

CAS号803712-67-6
分子式C20H19N3O
分子量 317.384
别名 GX15-070
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C
溶解度
动物实验配方

Tags: Obatoclax | GX15-070 | Apoptosis | Bcl-2 | Autophagy | AmBeed-信号通路专用抑制剂 | Obatoclax 纯度/质量文件 | Obatoclax 亚型比较 | Obatoclax 生物活性 | Obatoclax 细胞研究 | Obatoclax 动物研究 | Obatoclax 临床数据 | Obatoclax 参考文献 | Obatoclax 实验方案 | Obatoclax 技术信息

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