Molecular Formula | C31H29Cl2F2N3O4 |
Molar Mass | 616.48 |
Density | 1.40±0.1 g/cm3(Predicted) |
Melting Point | >261° (dec.) |
Boling Point | 737.3±60.0 °C(Predicted) |
Solubility | DMSO (Slightly), Methanol (Slightly) |
Appearance | Form Solid, color White to Off-White |
Color | White to Off-White |
pKa | 4.11±0.10(Predicted) |
Storage Condition | -20°C Freezer |
Physical and Chemical Properties | Bioactive Idasanutlin (RG-7388) is a potent selective p53-MDM2 inhibitor with an IC50 of 6 nM. Its in vitro binding force, potency and selectivity in cells have been greatly improved. |
Use | Bioactive Idasanutlin (RG-7388) is a potent selective p53-MDM2 inhibitor with an IC50 of 6 nM. Its in vitro binding force, potency and selectivity in cells have been greatly improved. |
In vitro study | In cancer cells expressing wild-type p53, Idasanutlin inhibited cell proliferation with an IC50 of 30 nM and dose-dependently induced p53 stabilization, cell cycle arrest, and apoptosis. |
In vivo study | In the mouse SJSA human osteosarcoma xenograft model, Idasanutlin (25 mg/kg p.o.) inhibited tumor growth and allowed regression. In the SJSA xenograft model, Idasanutlin induces apoptosis and is anti-proliferative. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.622 ml | 8.111 ml | 16.221 ml |
5 mM | 0.324 ml | 1.622 ml | 3.244 ml |
10 mM | 0.162 ml | 0.811 ml | 1.622 ml |
5 mM | 0.032 ml | 0.162 ml | 0.324 ml |
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. |
Solubility | DMSO (Slightly), Methanol (Slightly) |