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- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
A-1210477
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
1668553-26-1
- 规格：
100mg/50mg/10mg/1mg/25mg/5mg
| 规格： | 100mg | 产品价格： | ￥5490.0 |
|---|---|---|---|
| 规格： | 50mg | 产品价格： | ￥3490.0 |
| 规格： | 10mg | 产品价格： | ￥1190.0 |
| 规格： | 1mg | 产品价格： | ￥256.0 |
| 规格： | 25mg | 产品价格： | ￥1990.0 |
| 规格： | 5mg | 产品价格： | ￥690.0 |
| 基本信息 | |
| CAS | No.1668553-26-1 |
| 英文名称 | A-1210477 |
| 别名 | Abbvie Mcl-1 Inhibitor |
| 分子式 | C46H55N7O7S |
| 分子量 | 850.04 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD28399118 |
| SMILES | O=C(C(N1CCN2CCOCC2)=C(CCCOC3=C4C=CC=CC4=CC=C3)C5=C1C(C6=C(COC7=CC=C(N8CCN(S(=O)(N(C)C)=O)CC8)C=C7)N(C)N=C6C)=CC=C5)O |
| 靶点 | Mcl-1 |
| 通路 | Apoptosis |
| 背景说明 | A-1210477是一种有效的选择性MCL-1抑制剂。 |
| 生物活性 | A-1210477 is a potent and selective inhibitor of MCL-1 with a Ki of 0.45 nM[1]. A-1210477 specifically binds MCL-1 and promotes apoptosis of cancer cells in an MCL-1-dependent manner[2]. |
| In Vitro | A-1210477(10μM)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<10μM，confirming that A-1210477 can kill MCL-1-dependent cell lines[1]. |
| 细胞实验 | 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.[1] |
| 激酶实验 | 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 340/35nm excitation filter and 520/525(f-Bak)and 495/510nm(Tb-labeled anti-GST antibody)emission filters.[1] |
| 数据来源文献 | [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. [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. |
| 单位 | 瓶 |
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IA2520 A-1210477 抑制剂/拮抗剂/激动剂 索莱宝
￥256 - 5490
