化学性质:
规格 | 10 mM * 1 mL in DMSO 5mg 10mg 50mg 100mg |
CAS | 130 |
别名 | N/A |
化学名 | (2'R,3S,4'S,5'R,Z)-6-chloro-4'-(3-chloro-2-fluorophenyl)-2-hydroxy-N-((1r,4R)-4-hydroxycyclohexyl)-2'-neopentylspiro[indole-3,3'-pyrrolidine]-5'-carbimidic acid |
分子式 | C29H34Cl2FN3O3 |
分子量 | 562.5 |
溶解度 | Soluble in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
MI-773 is a small molecule inhibitor of MDM2 with IC50 value of 62nM [1].
MI-773 is a small molecule MDM2 antagonist. It is a spirooxindole derivative. MI-773 shows a high MDM2 affinity with IC50 value of 62nM in the FP competitive binding experiment. In the in vitro cell-based assay, MI-773 shows a similar inhibition efficacy with its enantiomer MI-77301. The GI50 values are 58nM and 33nM for MI-773 and MI-77301, respectively. Both MI-773 and MI-77301 exert considerable activity at dose of 100 mg/kg in mouse xenograft models of osteosarcoma, prostate cancer, colorectal cancer, leukemia or melanoma. Currently, an international and multicenter phase I trial of MI-773 is underway for patients with liposarcomas and other p53-wild-type tumors [1, 2].
References:
[1] Zak K, Pecak A, Rys B, Wladyka B, D?mling A, Weber L, Holak TA, Dubin G. Mdm2 and MdmX inhibitors for the treatment of cancer: a patent review (2011-present). Expert Opin Ther Pat. 2013 Apr;23(4):425-48.
[2] Shoushtari AN, Van Tine BA, Schwartz GK. Novel treatment targets in sarcoma: more than just the GIST. Am Soc Clin Oncol Educ Book. 2014:e488-95.
特别提醒:
1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。
2. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。
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