A-1210477
作者：齊岳
發(fā)布時間：2023-08-30
09:02:51
點擊數(shù)：
產(chǎn)品名稱：A-1210477
產(chǎn)品描述：
| 產(chǎn)品描述 | A-1210477 is an effective and specific MCL-1 and Bcl-2 inhibitor (Ki/IC50: 0.454/26.2 nM). |
| 靶點活性 | MCL-1:26.2 nM |
| 體外活性 | In H929 cells, A-1210477 binds to MCL-1 with high affinity and induces MCL-1 protein elevation. In H929, H2110, and H23 cells, A-1210477 induce the hallmarks of apoptosis, and inhibits MCL-1-dependent cell viability. A-1210477 also synergizes with navitoclax to kill a variety of cancer cell lines. [1] In SKBR3 cells, A-1210477 inhibits MCL-1–BIM interaction and induces classical features of apoptosis. [2] In addition, A-1210477 sensitizes non-Hodgkin's lymphoma cell lines to venetoclax (ABT-199). [3] |
| 激酶實驗 | Binding affinity assays: 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 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. |
| 細(xì)胞實驗 | 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 were seeded at 15?000–20?000 cells per well and treated similarly. Effects on proliferation and viability were determined using CellTiter-Glo reagent according to the manufacturer's instructions. IC50 values are determined by non-linear regression analysis of the concentration response data.(Only for Reference) |
| 分子量 | 850.04 |
| 分子式 | C46H55N7O7S |
| CAS No. | 1668553-26-1 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: Insoluble
H2O: 10 mM
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齊岳生物科技有限公司是集化學(xué)科研和定制與一體的高科技化學(xué)公司。業(yè)務(wù)范圍包括化學(xué)試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學(xué)品、中間體和化工材料等領(lǐng)域。
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