MI-1061 TFA |
| Katalog-Nr.GC62598 |
MI-1061 TFA ist ein potenter, oral bioverfÜgbarer und chemisch stabiler MDM2-Inhibitor (MDM2-p53-Interaktion) (IC50 = 4,4 nM; Ki = 0,16 nM). MI-1061 TFA aktiviert stark p53 und induziert Apoptose im SJSA-1-Xenotransplantat-Tumorgewebe in MÄusen. Anti-Tumor-AktivitÄt.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1410737-35-7
Sample solution is provided at 25 µL, 10mM.
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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].
[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.
Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)
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