| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| M421181-1ml |
1ml |
期货  |
|
| 英文别名 | SAR405838 | 1303607-60-4 | MI-77301 | SAR-405838 | MI-773 (SAR405838) | 8570LZ3RCA | CHEMBL2381408 | (2'S,3R,4'S,5'R)-6-Chloro-4'-(3-chloro-2-fluorophenyl)-2'-(2,2-dimethylpropyl)-N-(trans-4-hydroxycyclohexyl)-2-oxo-1,2-dihydrospiro(indole-3,3'-pyrrolidine)-5'-carboxam |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | MI-773 (SAR405838) |
| 生化机理 | MI-773 (SAR405838) 是一种口服 MDM2 拮抗剂，Ki值为 0.88 nM。第一阶段 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
MI-773 (SAR405838) 是一种口服生物有效的MDM2拮抗剂，Ki为0.88 nM。Phase 1。 应用 SAR405838 是 MI-773 的类似物，具有抗肿瘤活性。它是一种高效、选择性的Mdm2-p53相互作用抑制剂，与 Mdm2 结合的Ki值为 0.88 nM。 Information MI-773 (SAR405838) MI-773 (SAR405838) is an orally available MDM2 antagonist with K i of 0.88 nM. Phase 1. Targets p53 ; MDM2 (Cell-free assay) ; 0.88 nM(Ki) In vitro MI-773 binds to MDM2 with Ki of 0.88 nM. MI-773 potently inhibits cell growth in cancer cell lines, including SJSA-1 (IC50, 0.092 μM), RS4;11 (IC50, 0.089 μM), LNCaP (IC50, 0.27 μM), and HCT-116 (IC50, 0.20 μM) cells, and displays high selectivity over cancer cell lines with mutated or deleted p53, including SAOS-2 (IC50, >10 μM), PC-3 (IC50, >10 μM), SW620 (IC50, >10 μM), and HCT-116 (p53-/-) (IC50, >20 μM) cells. In vivo In the SJSA-1 osteosarcoma, acute lymphoblastic leukemia RS4;11, LNCaP prostate cancer, and HCT-116 colon cancer xenograft model, MI-773 (p.o.) effectively inhibits tumor growth in a dose-dependent manner (10 mg/kg, 30 mg/kg, 50 mg/kg, 100 mg/kg, and 200 mg/kg,). Cell Research(from reference) Cell lines：SJSA-1, RS4;11, LNCaP, SAOS-2, PC-3, SW620, HCT-116, and HCT-116 (p53-/-) cells Concentrations：100 μM Incubation Time：~48 h |
| 分子类型 | 小分子 |
|---|---|
| IIUPAC Name | (2'R,3R,3'S,5'S)-6-chloro-3'-(3-chloro-2-fluorophenyl)-5'-(2,2-dimethylpropyl)-N-(4-hydroxycyclohexyl)-2-oxospiro[1H-indole-3,4'-pyrrolidine]-2'-carboxamide |
| INCHI | 1S/C29H34Cl2FN3O3/c1-28(2,3)14-22-29(19-12-7-15(30)13-21(19)34-27(29)38)23(18-5-4-6-20(31)24(18)32)25(35-22)26(37)33-16-8-10-17(36)11-9-16/h4-7,12-13,16-17,22-23,25,35-36H,8-11,14H2,1-3H3,(H,33,37)(H,34,38)/t16?,17?,22-,23-,25+,29+/m0/s1 |
| InChi Key | IDKAKZRYYDCJDU-AEPXTFJPSA-N |
| Smiles | CC(C)(C)CC1C2(C(C(N1)C(=O)NC3CCC(CC3)O)C4=C(C(=CC=C4)Cl)F)C5=C(C=C(C=C5)Cl)NC2=O |
| Isomeric SMILES | CC(C)(C)C[C@H]1[C@@]2([C@H]([C@@H](N1)C(=O)NC3CCC(CC3)O)C4=C(C(=CC=C4)Cl)F)C5=C(C=C(C=C5)Cl)NC2=O |
| 分子量 | 562.5 |
| Reaxy-Rn | 32303642 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=32303642&ln= |
| 分子量 | 562.500 g/mol |
|---|---|
| XLogP3 | 5.300 |
| 氢键供体数Hydrogen Bond Donor Count | 4 |
| 氢键受体数Hydrogen Bond Acceptor Count | 5 |
| 可旋转键计数Rotatable Bond Count | 5 |
| 精确质量Exact Mass | 561.196 Da |
| 单同位素质量Monoisotopic Mass | 561.196 Da |
| 拓扑极表面积Topological Polar Surface Area | 90.500 Ų |
| 重原子数Heavy Atom Count | 38 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 895.000 |
| 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 | 4 |
| 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 |
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