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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:
S63845
- 库存:
999
- 供应商:
北京索莱宝科技有限公司
- CAS号:
1799633-27-4
- 规格:
1mg/5mg/10mg
| 规格: | 1mg | 产品价格: | ¥980.00 |
|---|---|---|---|
| 规格: | 5mg | 产品价格: | ¥2790.00 |
| 规格: | 10mg | 产品价格: | ¥4470.00 |
| CAS | 1799633-27-4 |
| 英文名称 | S63845 |
| 别名 | ;S63845;S-63845;GinsenosideRg3; |
| 分子式 | C39H37ClF4N6O6S |
| 分子量 | 829.26 |
| 规格 | 1mg ; 5mg ; 10mg |
| 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 |
| 运输条件 | 冷藏运输 |
| 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 |
| InChIKey | ZFBHXVOCZBPADE-UHFFFAOYSA-N |
| InChI | InChI=1S/C39H37ClF4N6O6S/c1-23-26(7-8-28(34(23)40)53-18-17-49-15-13-48(2)14-16-49)32-33-36(45-22-46-37(33)57-35(32)29-9-10-31(41)55-29)56-30(38(51)52)19-24-5-3-4-6-27(24)54-20-25-11-12-47-50(25)21-39(42,43)44/h3-12,22,30H,13-21H2,1-2H3,(H,51,52) |
| PubChem CID | 126970642 |
| 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]. |
| In Vivo | 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 |
| 表格1 | |*|1mg|5mg|10mg|$$|1mM|1.2059mL|6.0295mL|12.0589mL|$$|5mM|0.2412mL|1.2059mL|2.4118mL|$$|10mM|0.1206mL|0.6029mL|1.2059mL| |

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文献和实验S-腺苷甲硫氨酸 S- adenosylmethionine 亦称活性甲硫氨酸,在生物体内由 ATP与甲硫氨酸在甲硫氨酸活化酶的作用下合成。甲硫键是高能键,另外其丙基胺部分也加入到多胺化合物中。当胆碱、肌酸及其它甲基化合物生成时它作为甲基供体而起作用。认为甲硫氨酸的分解也经过此物质。
Summary: Illumina's Solexa Sequencing Technology
Here I present a brief overview of Solexa's sequencing-by-synthesis chemistry. The sample prep methods used differ slightly from that used in ABI's SOLiD system, but the basic goals are the same: generate large numbers of unique "polonies
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