MI-1061

Modify Date: 2024-01-09 23:13:22

MI-1061 Structure
MI-1061 structure
Common Name MI-1061
CAS Number 1410737-34-6 Molecular Weight 582.45
Density N/A Boiling Point N/A
Molecular Formula C30H26Cl2FN3O4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of MI-1061


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, induces apoptosis, and has anti-tumor activity[1].

 Names

Name MI-1061

 MI-1061 Biological Activity

Description 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, induces apoptosis, and has anti-tumor activity[1].
Related Catalog
Target

IC50: 4.4 nM (MDM2)[1] Ki: 0.16 nM (MDM2)

In Vitro 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].
In Vivo MI-1061 is capable of achieving tumor regression in the SJSA-1 xenograft tumor model in mice with oral administration[1].
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.

 Chemical & Physical Properties

Molecular Formula C30H26Cl2FN3O4
Molecular Weight 582.45