S63845产品图

S63845

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  • ¥980 - 4470
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  • 北京
  • IS1680
  • 2026年08月13日
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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

      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
    CAS1799633-27-4
    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
    MDLMFCD31382374
    SMILESCC(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
    InChIKeyZFBHXVOCZBPADE-UHFFFAOYSA-N
    InChIInChI=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 CID126970642
    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]
    IC50MCL1 0.19 nM (Kd)[1]
    In VitroThe 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 VivoS63845 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
    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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    图标文献和实验
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    • 鹅〔脱氧〕胆酸 s chenodeoxycholic acid

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