product description | Idasanutlin(RG7388) is an effective selective MDM2 antagonist, inhibiting p53-MDM2 binding, IC50 is 6 nM. |
in vitro action | Idasanutlin(RG7388) inhibits cell proliferation with an IC50 of 30 nM and induces dose-dependent p53 stabilization, cell cycle arrest and apoptosis of cancer cells expressing wild-type p53. Idasanutlin(RG7388)(300 nM or 1.8 μM) induced apoptosis in SJSA osteosarcoma cells. |
in vivo action | in mouse SJSA human osteosarcoma xenograft model, Idasanutlin(RG7388,25 mg / kg p.o.) leads to tumor growth inhibition and regression. In the SJSA xenograft model, Idasanutlin(RG7388) induced apoptosis and antiproliferation. |
biological activity | Idasanutlin (RG-7388) is an effective selective p53-MDM2 inhibitor with an IC50 of 6 nM. Its in vitro binding force, potency and selectivity in cells have been greatly improved. |
target | TargetValue Mdm2 (Cell-free say) 6 nM |
Target | Value |
Mdm2
(Cell-free assay)
| 6 nM |
in vitro study | in cancer cells expressing wild-type p53, Idasanutlin inhibit cell proliferation with IC50 of 30 nM, and induce p53 stabilization, cell cycle arrest and cell apoptosis in a dose-dependent manner. |
in vivo study | in mouse SJSA human osteosarcoma xenograft model, Idasanutlin (25 mg/kg p.o.) inhibited tumor growth and made it regress. In the SJSA xenograft model, Idasanutlin induces apoptosis and resists proliferation. |