ABT-737

目录号: HY-50907 纯度: 99.96%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

ABT-737 是一种 BH3 模拟物，是一种有效的 Bcl-2、Bcl-x_L 和 Bcl-w 抑制剂，EC₅₀ 分别为 30.3 nM、78.7 nM 和 197.8 nM。ABT-737 诱导 BCL-2/BAX 复合物的破坏和 BAK 依赖性但不依赖 BIM 的内在凋亡途径激活。ABT-737 诱导自噬，并且具有用于急性髓系白血病 (AML) 研究的潜力。

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ABT-737 Chemical Structure

CAS No. : 852808-04-9

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥805	In-stock
5 mg	￥750	In-stock
10 mg	￥900	In-stock
50 mg	￥3000	In-stock
100 mg	￥5300	In-stock
200 mg	现货	询价
500 mg		询价
1 g		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of ABT-737:

ABT-737-d₈ In-stock

MCE 顾客使用本产品发表的 45 篇科研文献

: ABT-737 purchased from MCE. Usage Cited in: Cancer Lett. 2019 Oct 1;461:102-111. [Abstract]; Expression of active (cleaved) PARP and active (cleaved) Caspase-3 after 48h of treatment with AGS, 1 μM ABT-737 or 1 μM ABT-737 added to AGS as determined by Western blot. Floating cells are included in lysate.

ABT-737 相关产品

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-x_L and Bcl-w inhibitor with EC₅₀s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research^[1]^[2]^[3].

IC₅₀ & Target^[1]

Bcl-2

30.3 nM (EC₅₀)

Bcl-xL

78.7 nM (EC₅₀)

Bcl-W

197.8 nM (EC₅₀)

Bcl-B

1820 nM (EC₅₀)

Bfl-1

>10 μM (EC₅₀)

Mcl-1

>10 μM (EC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
CCRF-CEM	IC₅₀	0.74 μM Compound: 1, ABT-737	Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay	[PMID: 22582991]
DU-145	IC₅₀	27.6 μM Compound: 7, ABT-737	Cytotoxicity against human DU145 cells after 48 hrs by cell titer-blue assay Cytotoxicity against human DU145 cells after 48 hrs by cell titer-blue assay	[PMID: 19743858]
FL5.12	EC₅₀	30 nM Compound: 1, ABT-737	Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl-XL assessed as cell viability after 24 hrs by MTS assay in absence of serum Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl-XL assessed as cell viability after 24 hrs by MTS assay in absence of serum	[PMID: 18841882]
FL5.12	EC₅₀	7.7 nM Compound: 1, ABT-737	Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl2 assessed as cell viability after 24 hrs by MTS assay in absence of serum Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl2 assessed as cell viability after 24 hrs by MTS assay in absence of serum	[PMID: 18841882]
HCT-116	IC₅₀	4.06 μM Compound: 7, ABT-737	Cytotoxicity against human HCT116 cells after 48 hrs by cell titer-blue assay Cytotoxicity against human HCT116 cells after 48 hrs by cell titer-blue assay	[PMID: 19743858]
HCT-116	IC₅₀	47.7 μM Compound: ABT-737	Cytotoxicity against human HCT116 cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay	[PMID: 22172701]
HL-60	IC₅₀	0.76 μM Compound: 1, ABT-737	Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by celltiter-blue assay Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by celltiter-blue assay	[PMID: 22582991]
HL-60	IC₅₀	0.97 μM Compound: ABT-737	Growth inhibition of human HL60 cells after 72 hrs by MTT assay Growth inhibition of human HL60 cells after 72 hrs by MTT assay	[PMID: 27712939]
Jurkat	IC₅₀	1.38 μM Compound: 7, ABT-737	Cytotoxicity against human Jurkat cells after 48 hrs by cell titer-blue assay Cytotoxicity against human Jurkat cells after 48 hrs by cell titer-blue assay	[PMID: 19743858]
K562	IC₅₀	16.4 μM Compound: ABT-737	Induction of apoptosis in Mcl1 dependent human K562 cells after 48 hrs by Annexin V staining based flow cytometry Induction of apoptosis in Mcl1 dependent human K562 cells after 48 hrs by Annexin V staining based flow cytometry	[PMID: 23314054]
K562	IC₅₀	34.7 μM Compound: 1, ABT-737	Cytotoxicity against human K562 cells assessed as cell viability after 48 hrs by celltiter-blue assay Cytotoxicity against human K562 cells assessed as cell viability after 48 hrs by celltiter-blue assay	[PMID: 22582991]
Leukemia cell	IC₅₀	> 1 μM Compound: 1, ABT-737	Binding affinity to human/mouse chimeric Mcl-1 by luminescence proximity assay Binding affinity to human/mouse chimeric Mcl-1 by luminescence proximity assay	[PMID: 23767404]
Leukemia cell	IC₅₀	> 10 μM Compound: 1, ABT-737	Binding affinity to human/mouse chimeric Mcl-1 by surface plasmon resonance assay Binding affinity to human/mouse chimeric Mcl-1 by surface plasmon resonance assay	[PMID: 23767404]
MCF7	IC₅₀	21.26 μM Compound: 7, ABT-737	Cytotoxicity against human MCF7 cells after 48 hrs by cell titer-blue assay Cytotoxicity against human MCF7 cells after 48 hrs by cell titer-blue assay	[PMID: 19743858]
MCF7	IC₅₀	25.33 μM Compound: ABT-737	Growth inhibition of human MCF7 cells after 72 hrs by MTT assay Growth inhibition of human MCF7 cells after 72 hrs by MTT assay	[PMID: 27712939]
MCF7	EC₅₀	4.39 μM Compound: ABT-737	Antiproliferative activity against cisplatin-resistant human MCF7-CR cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against cisplatin-resistant human MCF7-CR cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 35421577]
MDA-MB-435	IC₅₀	> 122.94 μM Compound: ABT-737	Cytotoxicity against human MDA-MB-435 cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-435 cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay	[PMID: 22172701]
MEF	EC₅₀	> 10000 nM Compound: 1, ABT-737	Cytotoxicity against mouse MEF cells expressing mcl-1 fl/fl after 24 hrs by Cell titer glo assay in presence of 1% serum Cytotoxicity against mouse MEF cells expressing mcl-1 fl/fl after 24 hrs by Cell titer glo assay in presence of 1% serum	[PMID: 21366295]
MEF	EC₅₀	> 10000 nM Compound: 1, ABT-737	Cytotoxicity against mouse MEF cells expressing mcl-1 fl/fl after 24 hrs by Cell titer glo assay in presence of 10% serum Cytotoxicity against mouse MEF cells expressing mcl-1 fl/fl after 24 hrs by Cell titer glo assay in presence of 10% serum	[PMID: 21366295]
MEF	EC₅₀	0.013 μM Compound: 1; ABT-737	Cytotoxicity against MCL deficient mouse embryonic fibroblast cells assessed as reduction in cell viability in presence of 1 % fetal calf serum measured after 24 hrs by propidium iodide staining based flow cytometric analysis Cytotoxicity against MCL deficient mouse embryonic fibroblast cells assessed as reduction in cell viability in presence of 1 % fetal calf serum measured after 24 hrs by propidium iodide staining based flow cytometric analysis	[PMID: 33904752]
MEF	EC₅₀	2.03 nM Compound: 1, ABT-737	Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 1% serum Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 1% serum	[PMID: 21366295]
MEF	EC₅₀	51 nM Compound: 1, ABT-737	Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% fetal bovine serum Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% fetal bovine serum	[PMID: 21366295]
MEF	EC₅₀	51 nM Compound: 1, ABT-737	Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% serum Cytotoxicity against mouse mcl-1 deficient MEF cells after 24 hrs by Cell titer glo assay in presence of 10% serum	[PMID: 21366295]
MOLT-4	IC₅₀	227 nM Compound: ABT-263	Antiproliferative activity against human MOLT-4 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay Antiproliferative activity against human MOLT-4 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay	[PMID: 32145645]
NCI-H1417	IC₅₀	0.13 μM Compound: 1, ABT-737	Growth inhibition of human NCI-H1417 cells after 4 days by WST8 assay Growth inhibition of human NCI-H1417 cells after 4 days by WST8 assay	[PMID: 22448988]
NCI-H1417	IC₅₀	173.4 nM Compound: 1, ABT-737	Cytotoxicity against human NCI-H1417 cells assessed as growth inhibition after 4 days by WST assay Cytotoxicity against human NCI-H1417 cells assessed as growth inhibition after 4 days by WST assay	[PMID: 23448298]
NCI-H1417	IC₅₀	412 nM Compound: 1, ABT-737	Antiproliferative activity against human NCI-H1417 cells after 4 days by WST8 assay Antiproliferative activity against human NCI-H1417 cells after 4 days by WST8 assay	[PMID: 22747598]
NCI-H146	EC₅₀	0.087 μM Compound: 1, ABT-737	Cytotoxicity against human NCI-H146 cells assessed as cell viability after 48 hrs in presence of 10% human serum Cytotoxicity against human NCI-H146 cells assessed as cell viability after 48 hrs in presence of 10% human serum	[PMID: 18841882]
NCI-H146	IC₅₀	0.097 μM Compound: 1, ABT-737	Growth inhibition of human NCI-H146 cells after 4 days by WST8 assay Growth inhibition of human NCI-H146 cells after 4 days by WST8 assay	[PMID: 22448988]
NCI-H146	IC₅₀	37 nM Compound: 1, ABT-737	Antiproliferative activity against human NCI-H146 cells after 4 days by WST8 assay Antiproliferative activity against human NCI-H146 cells after 4 days by WST8 assay	[PMID: 22747598]
NCI-H146	IC₅₀	43.8 nM Compound: ABT-263	Antiproliferative activity against human NCI-H146 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay Antiproliferative activity against human NCI-H146 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay	[PMID: 32145645]
NCI-H187	IC₅₀	137.7 nM Compound: 1, ABT-737	Cytotoxicity against human NCI-H187 cells assessed as growth inhibition after 4 days by WST assay Cytotoxicity against human NCI-H187 cells assessed as growth inhibition after 4 days by WST assay	[PMID: 23448298]
NCI-H1963	IC₅₀	54 nM Compound: 1, ABT-737	Cytotoxicity against human NCI-H1963 cells assessed as growth inhibition after 4 days by WST assay Cytotoxicity against human NCI-H1963 cells assessed as growth inhibition after 4 days by WST assay	[PMID: 23448298]
NCI-H1963	IC₅₀	59 nM Compound: 1, ABT-737	Antiproliferative activity against human NCI-H1963 cells after 4 days by WST8 assay Antiproliferative activity against human NCI-H1963 cells after 4 days by WST8 assay	[PMID: 22747598]
NCI-H23	IC₅₀	71.16 μM Compound: ABT-737	Growth inhibition of human NCI-H23 cells after 72 hrs by MTT assay Growth inhibition of human NCI-H23 cells after 72 hrs by MTT assay	[PMID: 27712939]
NCI-H460	IC₅₀	8.03 μM Compound: 7, ABT-737	Cytotoxicity against human H460 cells after 48 hrs by cell titer-blue assay Cytotoxicity against human H460 cells after 48 hrs by cell titer-blue assay	[PMID: 19743858]
Platelet	IC₅₀	242 nM Compound: ABT-263	Toxicity in human platelet assessed as reduction in cell viability measured after 48 hrs by MTS assay Toxicity in human platelet assessed as reduction in cell viability measured after 48 hrs by MTS assay	[PMID: 32145645]
Raji	IC₅₀	93.49 μM Compound: ABT-737	Cytotoxicity against human Raji cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay Cytotoxicity against human Raji cells expressing Bcl-xL, Bcl-2 and Mcl-1 after 72 hrs by MTT assay	[PMID: 22172701]
RS4-11	IC₅₀	0.27 μM Compound: ABT-737	Induction of apoptosis in Bcl2 dependent human RS4:11 cells after 48 hrs by Annexin V staining based flow cytometry Induction of apoptosis in Bcl2 dependent human RS4:11 cells after 48 hrs by Annexin V staining based flow cytometry	[PMID: 23314054]
RS4-11	IC₅₀	0.33 μM Compound: ABT-737	Cytotoxicity against human RS4:11 cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against human RS4:11 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 29453135]
RS4-11	IC₅₀	49 nM Compound: ABT-263	Antiproliferative activity against human RS4-11 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay Antiproliferative activity against human RS4-11 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay	[PMID: 32145645]
SK-OV-3	IC₅₀	46.59 μM Compound: ABT-737	Growth inhibition of human SKOV3 cells after 72 hrs by MTT assay Growth inhibition of human SKOV3 cells after 72 hrs by MTT assay	[PMID: 27712939]
SU.86.86	IC₅₀	4.24 μM Compound: 7, ABT-737	Cytotoxicity against human SU-8686 cells after 48 hrs by cell titer-blue assay Cytotoxicity against human SU-8686 cells after 48 hrs by cell titer-blue assay	[PMID: 19743858]
U-266	IC₅₀	27.35 μM Compound: ABT-737	Growth inhibition of human U266 cells after 72 hrs by MTT assay Growth inhibition of human U266 cells after 72 hrs by MTT assay	[PMID: 27712939]

体外研究
(In Vitro)

ABT-737 与 BCL-2、BCL-X_L 和 BCL-W 具有高亲和力 (K_i<1 nM)，但与其他抗凋亡 BCL-2 家族成员（包括 MCL-1 和 BFL-1）的结合力较弱 (K_i>460 nM)。ABT-737 与 BCL-X_L 和 BCL-2 的 BH3 结合槽结合^[1]。
ABT-737（100 nM；1-72 小时）诱导 HL-60 细胞凋亡并与化疗产生协同作用^[1]。
ABT-737（5、7.5、10 μM；72 小时）导致约 80% 的 HCT116 细胞死亡。BAX 敲除变体对 ABT-737 具有完全抗性^[1]。
ABT-737 对细胞周期分布没有影响。ABT-737 破坏 BCL-2/BAX 异二聚化并诱导 HL-60 白血病细胞中的 BAX 构象变化^[1]。
ABT-737 可诱导敏感细胞中 BAX/BAK 依赖性最大 O₂ 消耗率受损。MCF10A 细胞中稳定的 BCL-2 过表达可诱导 ABT-737 敏感的死亡状态。ABT-737 可诱导 B 细胞淋巴瘤细胞中剂量依赖性最大 O₂ 消耗率受损^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

ABT-737（20、30 mg/kg/天；腹腔注射；持续 21 天）在 20 和 30 mg/kg 剂量水平下分别可抑制 4 至 6 周龄 CB.17 Scid 小鼠（患有人类白血病 KG-1 细胞）的白血病负担 48% 和 53%^[1]。
ABT-737 显著延长了这种恶性白血病模型中小鼠的生存期^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

813.43

Formula

C₄₂H₄₅ClN₆O₅S₂

CAS 号

852808-04-9

性状

固体

颜色

Yellow to orange

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 50 mg/mL (61.47 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.2294 mL	6.1468 mL	12.2936 mL
5 mM	0.2459 mL	1.2294 mL	2.4587 mL
10 mM	0.1229 mL	0.6147 mL	1.2294 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 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，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制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

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (3.07 mM); 悬浊液; 超声助溶

此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (3.07 mM); 悬浊液; 超声助溶

此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.07 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
方案四

请依序添加每种溶剂： 2% DMSO 40% PEG300 5% Tween-80 53% Saline
Solubility: 2 mg/mL (2.46 mM); 悬浊液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.96%

选择批次：

Data Sheet (656 KB) SDS (393 KB)

COA (194 KB) HNMR (324 KB) LCMS (256 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Konopleva M, et al. Mechanisms of apoptosis sensitivity and resistance to the BH3 mimetic ABT-737 in acute myeloid leukemia. Cancer Cell. 2006 Nov;10(5):375-88. [Content Brief]

[2]. Ahamed Saleem, et al. Effect of dual inhibition of apoptosis and autophagy in prostate cancer. Prostate. 2012 Sep 1;72(12):1374-81. [Content Brief]

[3]. Clerc P, et al. Polster BM.Rapid Detection of an ABT-737-Sensitive Primed for Death State in Cells Using Microplate-Based Respirometry.PLoS One. 2012;7(8):e42487. Epub 2012 Aug 3. [Content Brief]

Kinase Assay ^[1]	To determine the binding affinity of GST-BCL-2 family proteins to the FITC-conjugated BH3 domain of BIM (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR), FPAs are performed as follows. Briefly, 100 nM of GST-BCL-2 family fusion proteins are incubated with serial dilutions of ABT-737 in PBS for 2 min. Then, 20 nM of FITC-BIM BH3 peptide (FITC-Ahx-DMRPEIWIAQELRRIGDEFNAYYAR) is added. Fluorescence polarization is measured using an Analyst TM AD Assay Detection System after 10 min using the 96-well black plate. IC₅₀s are determined using GraphPad Prism software. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[3]	Cells are treated with ABT-737, ABT-263, or vehicle (DMSO) for 4 h in XF24 assay medium (6×10⁴ MCF10A cells, see medium composition below) or RPMI 1640 medium (1×10⁶ B-cell lymphoma cells) and apoptosis is analyzed by Annexin-V-binding/PI exclusion or by sub-diploid nuclei determination. FACS analysis is performed on Becton Dickinson FACScan or FACScalibur instruments. Data analysis is performed with CellQuest software. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	For intraperitoneal (i.p.) administration, 1 g/mL stock solution of ABT-737 in DMSO is added to a mixture of 30% propylene glycol, 5% Tween 80, 65% D5W (5% dextrose in water) (pH 4−5; final concentration of DMSO ≤ 1%). Mice injected with FD/ΔRaf-1:ER cells are treated with either ABT-737 (20 and 30 mg/kg/mouse every day i.p. for 21 days starting on day 1 post-cell injection (n=9-10 mice per group) or vehicle or left untreated (control); mice injected with human KG-1 cells are treated with 30 mg/kg ABT-737 starting on day 18 post-cell injection. For noninvasive imaging of FD/ΔRaf-1:ER-luc cells, anesthetized mice are injected with 150 mg/kg of D-luciferin and placed for imaging in the In Vivo Imaging System with total imaging time of 2 min. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Konopleva M, et al. Mechanisms of apoptosis sensitivity and resistance to the BH3 mimetic ABT-737 in acute myeloid leukemia. Cancer Cell. 2006 Nov;10(5):375-88. [Content Brief] [2]. Ahamed Saleem, et al. Effect of dual inhibition of apoptosis and autophagy in prostate cancer. Prostate. 2012 Sep 1;72(12):1374-81. [Content Brief] [3]. Clerc P, et al. Polster BM.Rapid Detection of an ABT-737-Sensitive Primed for Death State in Cells Using Microplate-Based Respirometry.PLoS One. 2012;7(8):e42487. Epub 2012 Aug 3. [Content Brief]

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完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.2294 mL	6.1468 mL	12.2936 mL	30.7341 mL
	5 mM	0.2459 mL	1.2294 mL	2.4587 mL	6.1468 mL
	10 mM	0.1229 mL	0.6147 mL	1.2294 mL	3.0734 mL
	15 mM	0.0820 mL	0.4098 mL	0.8196 mL	2.0489 mL
	20 mM	0.0615 mL	0.3073 mL	0.6147 mL	1.5367 mL
	25 mM	0.0492 mL	0.2459 mL	0.4917 mL	1.2294 mL
	30 mM	0.0410 mL	0.2049 mL	0.4098 mL	1.0245 mL
	40 mM	0.0307 mL	0.1537 mL	0.3073 mL	0.7684 mL
	50 mM	0.0246 mL	0.1229 mL	0.2459 mL	0.6147 mL
	60 mM	0.0205 mL	0.1024 mL	0.2049 mL	0.5122 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ABT-737852808-04-9ABT737ABT 737Bcl-2 FamilyApoptosisAutophagyMitophagyMitochondrial AutophagyBH3mimeticBCL-2/BAXBIMAMLHL-60HCT116Inhibitorinhibitorinhibit

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ABT-737

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