(2'R,3S,4'S,5'R)-6-氯-4'-(3-氯-2-氟苯基)-2'-(2,2-二甲基丙基)-1,2-二氢-N-(反式-4-羟基环己基)-2-氧代螺[3H-吲哚-3,3'-吡咯烷]-5'-甲酰胺
- CAS号:1303607-07-9
- 英文名:MI-773
- 中文名:(2'R,3S,4'S,5'R)-6-氯-4'-(3-氯-2-氟苯基)-2'-(2,2-二甲基丙基)-1,2-二氢-N-(反式-4-羟基环己基)-2-氧代螺[3H-吲哚-3,3'-吡咯烷]-5'-甲酰胺
- CBNumber:CB12685929
- 分子式:C29H34Cl2FN3O3
- 分子量:562.5
- MOL File:1303607-07-9.mol
- 沸点 :732.1±60.0 °C(Predicted)
- 密度 :1.36±0.1 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :Soluble in DMSO
- 形态 :Solid
- 酸度系数(pKa) :12.03±0.70(Predicted)
- 颜色 :White to off-white
(2'R,3S,4'S,5'R)-6-氯-4'-(3-氯-2-氟苯基)-2'-(2,2-二甲基丙基)-1,2-二氢-N-(反式-4-羟基环己基)-2-氧代螺[3H-吲哚-3,3'-吡咯烷]-5'-甲酰胺性质、用途与生产工艺
- 生物活性 MI-773 是一种 MDM2-p53 相互作用抑制剂,高亲和力结合到 MDM2,Ki 为 0.88 nM。
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靶点
Ki: 0.88 nM (MDM2)
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体外研究
MI-773 potently induces expression of p53 and its downstream targets p21, MDM2, and induces phosphorylation of p53 (serine 392) in low passage primary human ACC cells. Notably, MI-773 induces a dose-dependent increase in the fraction of apoptotic ACC cells and in the fraction of cells in the G1 phase of cell cycle (P<0.05). Consequently, MI-773 causes apoptotic cell death. MI-773 is an advanced synthetic small molecule inhibitor, displays high binding affinity against MDM2 (K d =8.2 nM).
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体内研究
MI-773 at 10 mg/kg modestly reduces the rate of tumor growth, whereas 100 mg/kg causes significant tumor regression. Control tumors reach an average of 1,000 mm 3 at 20 days of treatment, compare to an average volume of 600 mm 3 for the 10 mg/kg group and 30 mm 3 for the 100 mg/kg group. Kaplan-Meier analysis shows an increase in tumor failure, define as two times increase in tumor volume as compared to pretreatment volume (P=0.044), for vehicle-treated mice when compare to mice treated with 100 mg/kg MI-773.
- 更新日期:2024/11/08
- 产品编号:HY-17493
- 产品名称:MI-773
- CAS编号:
- 包装:1 mg
- 价格:727元
- 更新日期:2024/11/08
- 产品编号:HY-17493
- 产品名称:(2'R,3S,4'S,5'R)-6-氯-4'-(3-氯-2-氟苯基)-2'-(2,2-二甲基丙基)-1,2-二氢-N-(反式-4-羟基环己基)-2-氧代螺[3H-吲哚-3,3'-吡咯烷]-5'-甲酰胺 MI-773
- CAS编号:1303607-07-9
- 包装:5mg
- 价格:1600元
- 公司名称:CLEARSYNTH LABS LTD.
- 联系电话:--
- 电子邮件:sales@clearsynth.com
- 国家:印度
- 产品数:6257
- 优势度:58