| Identification | Back Directory | [Name]
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]-, 2,2,2-trifluoroacetate (1:1) | [CAS]
1410737-35-7 | [Synonyms]
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]-, 2,2,2-trifluoroacetate (1:1) | [Molecular Formula]
C32H27Cl2F4N3O6 | [MOL File]
1410737-35-7.mol | [Molecular Weight]
696.48 |
| Chemical Properties | Back Directory | [storage temp. ]
4°C, protect from light | [solubility ]
DMSO : 120 mg/mL (172.30 mM; Need ultrasonic) | [form ]
Solid | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
MI-1061 TFA is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 TFA potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity[1]. | [Biological Activity]
MI-1061 TFA is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 TFA potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity[1].
MI-1061 achieves IC50=100 and 250 nM in the SJSA-1 and HCT-116 p53+/+ cell lines, respectively, and has IC50>10000 nM in the p53 knockout cell line HCT-116 p53-/-cell line[1].
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]. | [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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| [storage]
4°C, protect from light | [References]
[1]. Aguilar A, et al. Design of chemically stable, potent, and efficacious MDM2 inhibitors that exploit the retro-mannich ring-opening-cyclization reaction mechanism in spiro-oxindoles. J Med Chem. 2014;57(24):10486-10498. |
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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
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