A-1210477

目录号: HY-12468 纯度: 99.40%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

A-1210477 是一种有效，选择性的 MCL-1 抑制剂，K_i 值为 0.45 nM。A-1210477 特异性结合 MCL-1，并以 MCL-1 依赖性方式促进癌细胞凋亡 (apoptosis)。

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A-1210477 Chemical Structure

CAS No. : 1668553-26-1

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3. 试用装只面向终端客户。

规格	价格	是否有货
1 mg	￥266	In-stock
5 mg	￥700	In-stock
10 mg	￥1200	In-stock
25 mg	￥2000	In-stock
50 mg	￥3500	In-stock
100 mg	￥5500	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

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MCE 顾客使用本产品发表的 17 篇科研文献

: A-1210477 purchased from MCE. Usage Cited in: Clin Res Hepatol Gas. 2019 Jun;43(3):292-300. [Abstract]; S63845 and A-1210477 trigger apoptosis signaling and reduce the levels of putative stem biomarkers in HCC cell lines.

: A-1210477 purchased from MCE. Usage Cited in: Open Biol. 2016 Aug;6(8). pii: 160134. [Abstract]; Immunoblots showing affinity purification of GFP-tagged Mcl-1 in the presence of 2 μM A-1210477, and detection of co-purifying Bak.

A-1210477 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

A-1210477 is a potent and selective inhibitor of MCL-1 with a K_i of 0.45 nM^[1]. A-1210477 specifically binds MCL-1 and promotes apoptosis of cancer cells in an MCL-1-dependent manner^[2].

IC₅₀ & Target^[1]

Mcl-1

0.45 nM (Ki)

Bcl-2

132 nM (Ki)

Bfl-1

660 nM (Ki)

Bcl-W

2280 nM (Ki)

Apoptosis

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
HEK-293T	IC₅₀	> 20 μM Compound: A1210477	Cytotoxicity against HEK293T cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay Cytotoxicity against HEK293T cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay	[PMID: 34228434]
HeLa	IC₅₀	> 20 μM Compound: A1210477	Cytotoxicity against human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay Cytotoxicity against human HeLa cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay	[PMID: 34228434]
HL-60	IC₅₀	2.46 μM Compound: A1210477	Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay	[PMID: 34228434]
K562	IC₅₀	> 30 μM Compound: 4; A1210477	Antiproliferative activity against human K562 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay	[PMID: 34342996]
K562	IC₅₀	13.9 μM Compound: A-1210477	Cytotoxicity against human K562 cells after 24 hrs by MTT assay Cytotoxicity against human K562 cells after 24 hrs by MTT assay	[PMID: 32794745]
KMS-12-PE	IC₅₀	> 40 μM Compound: A-1210477	Cytotoxicity against human KMS-12-PE cells after 24 hrs by MTT assay Cytotoxicity against human KMS-12-PE cells after 24 hrs by MTT assay	[PMID: 32794745]
L-363	IC₅₀	11.8 μM Compound: A-1210477	Cytotoxicity against human L-363 cells after 24 hrs by MTT assay Cytotoxicity against human L-363 cells after 24 hrs by MTT assay	[PMID: 32794745]
LP-1	IC₅₀	10.6 μM Compound: A-1210477	Cytotoxicity against human LP-1 cells after 24 hrs by MTT assay Cytotoxicity against human LP-1 cells after 24 hrs by MTT assay	[PMID: 32794745]
MM1.S	IC₅₀	> 40 μM Compound: A-1210477	Cytotoxicity against human MM1.S cells after 24 hrs by MTT assay Cytotoxicity against human MM1.S cells after 24 hrs by MTT assay	[PMID: 32794745]
MV4-11	IC₅₀	1.55 μM Compound: 4; A1210477	Antiproliferative activity against human MV4-11 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay	[PMID: 34342996]
NCI-H23	IC₅₀	13.5 μM Compound: 4; A1210477	Antiproliferative activity against human NCI-H23 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H23 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay	[PMID: 34342996]
NCI-H929	IC₅₀	0.9 μM Compound: 4; A1210477	Antiproliferative activity against human NCI-H929 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H929 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay	[PMID: 34342996]
NCI-H929	IC₅₀	8.6 μM Compound: A-1210477	Cytotoxicity against human NCI-H929 cells after 24 hrs by MTT assay Cytotoxicity against human NCI-H929 cells after 24 hrs by MTT assay	[PMID: 32794745]
RS4-11	IC₅₀	7.31 μM Compound: A1210477	Cytotoxicity against human RS4-11 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay Cytotoxicity against human RS4-11 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK8 assay	[PMID: 34228434]
SK-BR-3	IC₅₀	4.31 μM Compound: 4; A1210477	Antiproliferative activity against human SK-BR-3 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human SK-BR-3 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay	[PMID: 34342996]

体外研究
(In Vitro)

A-1210477 (10 μM) reduces the amount of BIM co-immunoprecipitated with MCL-1 antibody, and triggers MCL-1 elevation in a variety of cancer cell lines, including the breast cancer cell line HCC-1806. A-1210477 inhibits MCL-1-NOXA interactions with an IC₅₀ of approximately 1 μM, while having no effect on BCL-2-BIM or BCL-XL-BCL-XS interactions. The NSCLC cell lines H2110 and H23 are sensitive to A-1210477 with cell viability IC₅₀<10 μM, confirming that A-1210477 can kill MCL-1-dependent cell lines^[1].

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

分子量

850.04

Formula

C₄₆H₅₅N₇O₇S

CAS 号

1668553-26-1

性状

固体

颜色

White to off-white

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 : 10 mg/mL (11.76 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	1.1764 mL	5.8821 mL	11.7642 mL
5 mM	0.2353 mL	1.1764 mL	2.3528 mL
10 mM	0.1176 mL	0.5882 mL	1.1764 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: ≥ 1 mg/mL (1.18 mM); 澄清溶液

此方案可获得 ≥ 1 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 10.0 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: 1 mg/mL (1.18 mM); 悬浊液; 超声助溶

此方案可获得 1 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 10.0 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: ≥ 1 mg/mL (1.18 mM); 澄清溶液

此方案可获得 ≥ 1 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 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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: 99.40%

选择批次：

Data Sheet (632 KB) SDS (393 KB)

COA (199 KB) LCMS (276 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Leverson JD, et al. Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax). Cell Death Dis. 2015 Jan 15;6:e1590. [Content Brief]

[2]. Qing Wang, et al. A-1210477, a selective MCL-1 inhibitor, overcomes ABT-737 resistance in AML. Oncol Lett. 2019 Nov;18(5):5481-5489. [Content Brief]

Kinase Assay ^[1]	TR-FRET-binding affinity assays are performed for BCL-2, BCL-XL, and MCL-1 in 4.52 mM monobasic potassium phosphate, 15.48 mM dibasic potassium phosphate, 1 mM sodium EDTA, 0.05% Pluronic F-68 detergent, 50 mM sodium chloride, and 1 mM DTT (pH 7.5) for BCL-XL.6 For MCL-1 assays, GST-tagged MCL-1 (1 nM) is mixed with 100 nM f-Bak, 1 nM Tb-labeled anti-GST antibody, and compound at room temperature (RT) for 60 min. Fluorescence is measured on an Envision plate reader using a 340/35 nm excitation filter and 520/525 (f-Bak) and 495/510 nm (Tb-labeled anti-GST antibody) emission filters. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Adherent cell lines are seeded at 50 000 cells per well in 96-well plates and treated for 48 h with compounds diluted in half-log steps starting at 30 μM and ending at 0.001 μM. Multiple myeloma cell lines are seeded at 15 000-20 000 cells per well and treated similarly. Effects on proliferation and viability are determined using CellTiter-Glo reagent from Promega according to the manufacturer's instructions. IC₅₀ values are determined by non-linear regression analysis of the concentration response data. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Leverson JD, et al. Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax). Cell Death Dis. 2015 Jan 15;6:e1590. [Content Brief] [2]. Qing Wang, et al. A-1210477, a selective MCL-1 inhibitor, overcomes ABT-737 resistance in AML. Oncol Lett. 2019 Nov;18(5):5481-5489. [Content Brief]

A-1210477 相关分类

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	1.1764 mL	5.8821 mL	11.7642 mL	29.4104 mL
	5 mM	0.2353 mL	1.1764 mL	2.3528 mL	5.8821 mL
	10 mM	0.1176 mL	0.5882 mL	1.1764 mL	2.9410 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:

A-12104771668553-26-1A1210477A 1210477Bcl-2 FamilyApoptosisInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

A-1210477

MCE 顾客使用本产品发表的 17 篇科研文献