MI-136 is an inhibitor of the menin-MLL protein-protein interaction (PPI), with an IC50 of 31 nM and a Kd of 23.6 nM. MI-136 shows to block AR signaling and has the potential for the study in castration-resistant tumors.
性状
Solid
体外研究(In Vitro)
MI-136 (0-20) exhibits IC50values of 5.59 μM, 7.15 μM, 5.37 μM and 19.76 μM in LNCaP, VCaP, 22rv1 and PNT2 cells.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay
Cell Line:
AR positive cell lines such as VCaP, LNCaP and 22RV1.
Concentration:
0-20 μM.
Incubation Time:
24 h.
Result:
Inhibited cell proliferation.
体内研究(In Vivo)
MI-136 exhibits T1/2 of 3.1 h after po administration.
MI-136 (40 mg/kg, ip) leads to a significant decrease in the growth of castration-resistant VCaP tumors.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
VCaP xenografts.
Dosage:
40 mg/kg.
Administration:
Intraperitoneal injection, 5 days a week.
Result:
Led to a significant decrease in the growth of castration-resistant VCaP tumors compared to vehicle controls.