| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| A420458-1ml |
1ml |
现货  |
|
| 别名 | 阿福瑞塞替尼 (GSK2110183) |
|---|---|
| 英文别名 | N-[(2S)-1-amino-3-(3-fluorophenyl)propan-2-yl]-5-chloro-4-(4-chloro-2-methylpyrazol-3-yl)thiophene-2-carboxamide | NSC829868 | NSC-829868 | GTPL7890 | Q27281976 | AC-35761 | ASB183 | ASB-183 | Afuresertib | 2-Thiophenecarboxamide, N-[(1S)-2-amino-1-[(3-fl |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Afuresertib (GSK2110183) |
| 生化机理 | Afuresertib（GSK2110183）是一种强效的口服生物活性 Akt 抑制剂，对 Akt1、Akt2 和 Akt3 的Ki值分别为 0.08 nM、2 nM 和 2.6 nM。第二阶段 |
| 储存温度 | 避光,-80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 丝氨酸/苏氨酸蛋白激酶 AKT 抑制剂 |
| 产品介绍 |
Information Afuresertib (GSK2110183) is a potent, orally bioavailableAktinhibitor withKiof 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2. Targets Akt1 (Cell-free assay); Akt2 (Cell-free assay); Akt3 (Cell-free assay) 0.08 nM(Ki); 2 nM(Ki); 2.6 nM(Ki) In vitro Afuresertib inhibits the kinase activity of the E17K AKT1 mutant protein with EC50 of 0.2 nM. Afuresertib shows a concentration-dependent effect on multiple AKT substrate phosphorylation levels, including GSK3b, PRAS40, FOXO and Caspase 9. Overall 65% of the hematological cell lines are sensitive to afuresertib (EC50 < 1 μM). Among tested solid tumor cell lines, 21% have EC50 < 1 μM in response to afuresertib. In vivo Mice bearing BT474 breast tumor xenografts are dosed with afuresertib (p.o.) at 10, 30 or 100 mg/kg daily which results in 8, 37 and 61% TGI, respectively. Mice bearing SKOV3 ovarian tumor xenografts are treated with 10, 30 and 100 mg/kg afuresertib which results in 23, 37 and 97% TGI, respectively. Cell Research(from reference) Cell lines：Hematological cell lines and solid tumor cell lines Concentrations：30 μM Incubation Time：72 h |
| IC50 | Akt2, Ki: 2 nM |
|---|---|
| ALogP | 3.884 |
| hba_count | 2 |
| HBD Count | 2 |
| Rotatable Bond | 6 |
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| 分子类型 | 小分子 |
|---|---|
| IIUPAC Name | N-[(2S)-1-amino-3-(3-fluorophenyl)propan-2-yl]-5-chloro-4-(4-chloro-2-methylpyrazol-3-yl)thiophene-2-carboxamide |
| INCHI | 1S/C18H17Cl2FN4OS/c1-25-16(14(19)9-23-25)13-7-15(27-17(13)20)18(26)24-12(8-22)6-10-3-2-4-11(21)5-10/h2-5,7,9,12H,6,8,22H2,1H3,(H,24,26)/t12-/m0/s1 |
| InChi Key | AFJRDFWMXUECEW-LBPRGKRZSA-N |
| Smiles | CN1C(=C(C=N1)Cl)C2=C(SC(=C2)C(=O)NC(CC3=CC(=CC=C3)F)CN)Cl |
| Isomeric SMILES | CN1C(=C(C=N1)Cl)C2=C(SC(=C2)C(=O)N[C@@H](CC3=CC(=CC=C3)F)CN)Cl |
| 分子量 | 427.32 |
| Reaxy-Rn | 38723994 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=38723994&ln= |
| 敏感性 | 对光线敏感 |
|---|---|
| DMSO(mg / mL) Max Solubility | 85 |
| DMSO(mM) Max Solubility | 198.9141627 |
| Water(mg / mL) Max Solubility | ＜1 |
| 分子量 | 427.300 g/mol |
| XLogP3 | 4.000 |
| 氢键供体数Hydrogen Bond Donor Count | 2 |
| 氢键受体数Hydrogen Bond Acceptor Count | 5 |
| 可旋转键计数Rotatable Bond Count | 6 |
| 精确质量Exact Mass | 426.048 Da |
| 单同位素质量Monoisotopic Mass | 426.048 Da |
| 拓扑极表面积Topological Polar Surface Area | 101.000 Ų |
| 重原子数Heavy Atom Count | 27 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 520.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 1 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 0 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
| 1. Li Ji, Anqi Deng, Huiying Chen, Shuangyan Guo, Pingyu Wang, Ruiyi Zhang, Wenyang Chen, Taotao Fan, Lijuan Jiang, Bing Shen. (2025) Role of Ca2+/calmodulin and PI3K/AKT signaling pathways and active ingredients of BaoTaiYin in treatment of recurrent miscarriage. Frontiers in Molecular Biosciences, 12 (1573294). [PMID:40201242] [10.3389/fmolb.2025.1573294] |
| 2. Li Ji, Ziying Jiao, Lin Zhang, Jia Shi, Qianqian Wan, Chunzhi Qian, Han Wang, Xiaoyan Cao, Bing Shen, Lijuan Jiang. (2024) Role of increased IGFBP2 in trophoblast cell proliferation and recurrent spontaneous abortion development: A pilot study. Physiological Reports, 12 (3): (e15939). [PMID:38316422] [10.14814/phy2.15939] |
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