| Identification | Back Directory | [Name]
MI-1061 | [CAS]
1410737-34-6 | [Synonyms]
MI-1061
Benzoic acid, 4-[[[(3'R,4'S,5'R)-6''-chloro-4'-(3-chloro-2-fluorophenyl)-1'',2''-dihydro-2''-oxodispiro[cyclohexane-1,2'-pyrrolidine-3',3''-[3H]indol]-5'-yl]carbonyl]amino]- | [Molecular Formula]
C30H26Cl2FN3O4 | [MOL File]
1410737-34-6.mol | [Molecular Weight]
582.45 |
| Chemical Properties | Back Directory | [Boiling point ]
808.2±65.0 °C(Predicted) | [density ]
1.51±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 300 mg/mL (515.07 mM) | [form ]
Solid | [pka]
4.22±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
MI-1061 is a novel Chemically Stable, Potent, and Efficacious MDM2 Inhibitor. | [Uses]
MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity[1]. | [in vivo]
MI-1061 (100 mg/kg; p.o.; daily for 14 days) is capable of achieving tumor regression in the SJSA-1 xenograft tumor model in mice[1]. | Animal Model: | SCID mice bearing SJSA-1 osteosarcoma xenografts[1] | | Dosage: | 100 mg/kg | | Administration: | P.o.; daily for 14 days | | Result: | Demonstrated strong antitumor activity and achieved significant tumor regression.
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| [References]
[1] Aguilar A, et al. Design of chemically stable, potent, and efficacious MDM2 inhibitors that exploit the retro-mannichring-opening-cyclization reaction mechanism in spiro-oxindoles. J Med Chem. 2014 Dec 26;57(24):10486-98. DOI:10.1021/jm501541j |
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| Company Name: |
cjbscvictory
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| Tel: |
13348960310 13348960310 |
| Website: |
www.weikeqi-biotech.com/ |
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