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- 详细信息
- 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：
S63845
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
1799633-27-4
- 规格：
10mg/5mg/1mg
| 规格： | 10mg | 产品价格： | ￥4470.0 |
|---|---|---|---|
| 规格： | 5mg | 产品价格： | ￥2790.0 |
| 规格： | 1mg | 产品价格： | ￥980.0 |
S63845是一种新型的、选择性的MCL-1抑制剂。
| 基本信息 | |
| CAS | No.1799633-27-4 |
| 英文名称 | S63845 |
| 别名 | ;S63845;S-63845;GinsenosideRg3; |
| 分子式 | C39H37ClF4N6O6S |
| 分子量 | 829.26 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | White to yellow Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD31382374 |
| SMILES | CC(C(Cl)=C(OCCN1CCN(C)CC1)C=C2)=[C@@]2[C@]3=C(C4=CC=C(F)O4)SC5=NC=NC(O[C@H](CC6=C(OCC7=CC=NN7CC(F)(F)F)C=CC=C6)C(O)=O)=C53 |
| 靶点 | Mcl-1 |
| 通路 | Apoptosis |
| 背景说明 | S63845是一种新型的、选择性的MCL-1抑制剂。 |
| 生物活性 | S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor with a Kd of 0.19 nM for human MCL1.[1] |
| IC50 | MCL1 0.19 nM (Kd)[1] |
| In Vitro | The pro-survival protein myeloid cell leukemia 1 (MCL1) is over expressed in many cancers. S63845 is a small molecule that specifically binds with high affinity to the BH3-binding groove of MCL1. S63845 potently kills MCL1-dependent cancer cells， including multiple myeloma， leukaemia and lymphoma cells， by activating the BAX/BAK-dependent mitochondrial apoptotic pathway. The activity of S63845 is next evaluated in a panel of eight AML cell lines: all lines are sensitive to S63845 (IC50=4-233 nM)[1]. |
| 细胞实验 | S63845 shows potent anti-tumour activity with an acceptable safety margin as a single agent in several cancers. Intravenously injected (i.v.) S63845 exerts dose-dependent anti-tumour activity in human multiple myeloma (H929 and AMO1) xenografts in immunocompromised mice， with maximal tumour growth inhibition of 114% in the AMO1 model and 103% in the H929 model. At 25 mg/kg， S63845 induces complete regression in 7 out of 8 of the mice at 100 days after treatment in the AMO1 model[1]. |
| 细胞实验 | Cells are treated with increasing doses of S63845 (typically 0.008， 0.025， 0.04， 0.2， 1， 5 μM) for 24 h. Cells are stained with Annexin V-FITC and propidium iodide， analysed on a FACS Calibur and live cells are recorded. Data are presented as per cent cell death induction relative to cells cultured in medium alone[1]. |
| 动物实验 | Mice: S63845 is formulated extemporaneously in 25 mM HCl， 20% 2-hydroxy propyl β -cyclo dextrin 20% and administrated at the 6.25， 12.5， 25 mg/kg for 0， 20， 40， 60， 80 days. Tumour growth inhibition (TGImax) is calculated[1]. |
| 激酶实验 | 10 mM HEPES pH 7.4， 175 mM NaCl， 25 μM EDTA， 1 mM TCEP， 0.01% P20 and 1% DMSO is used as a running buffer. The ligand surface is generated using double His-tagged proteins. Serial dilutions of the compound in buffer are injected over the protein surface. All sample measurements are performed at a flow rate of 30 μL per min (injection time 120 s， dissociation time 360 s). The sensor surface is regenerated by consecutive injections of 0.35 M EDTA pH 8.0 with 0.1 mg/mL trypsin， 0.5 M imidazole and 45% DMSO (60 s， 15 μL per min)[1]. |
| 数据来源文献 | [1]. Kotschy A， et al. The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models. Nature. 2016 Oct 27;538(7626):477-482. |
| 单位 | 瓶 |
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