Molecular Formula | C26H23N5O |
Molar Mass | 421.49 |
Density | 1.39 |
Melting Point | >175°C (dec.) |
Solubility | Soluble in DMSO (up to 30 mg/ml) |
Appearance | solid |
Color | Yellow |
pKa | 14.84±0.40(Predicted) |
Storage Condition | -20°C |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months. |
In vitro study | OSI-906 inhibited IGF-IR activation of autophosphorylation and downstream signaling proteins AKT, ERK1/2 and S6 kinase with an IC50 of 0.028 to 0.13 μm. OSI-906 the target protein forms an intermediate structural morphology by interacting with the C- helix. OSI-906 effect on liver microsomes, with good metabolic stability. OSI-906 concentration of 1 m, complete inhibition of IR and IGF-IR phosphorylation. OSI-906 inhibits proliferation of several tumor cell lines, including non-small cell lung cancer and colorectal cancer (CRC) tumor cell lines, with EC50 of 0.021 to 0.810 μm. OSI-906 inhibited IGF-IR activation of autophosphorylation and downstream signaling proteins AKT, ERK1/2 and S6 kinases with an IC50 of 0.028 to 0.13 μm. OSI-906 the target protein forms an intermediate structural morphology by interacting with the C- helix. OSI-906 effect on liver microsomes, with good metabolic stability. OSI-906 concentration of 1 m, complete inhibition of IR and IGF-IR phosphorylation. OSI-906 inhibits proliferation of several tumor cell lines, including non-small cell lung cancer and colorectal cancer (CRC) tumor cell lines, with EC50 of 0.021 to 0.810 μm. |
In vivo study | OSI-906 on IGF-IR-driven xenograft tumor mouse model, inhibit tumor growth, at a dose of 75 mg/kg treatment, resulting in 100% TGI and 55% decline, at a dose of 25 mg/kg treatment, results in 60% TGI, no regression. Treatment of dogs, rats and mice OSI-906 induced different elimination half-lives of 1.18 hours, 2.64 hours and 2.14 hours, respectively. OSI-906 female Sprague-Dawley rats and female CD-1 mice were treated individually at different doses, once a day, and the Vmax values were not proportional to the OSI-906 dose. OSI-906 according to the dose of 25 mg/kg treatment for 12 days, improve the blood sugar value. OSI-906 treatment of a IGF-IR-driven human full-length human IGF-IR (LISN) transplanted mouse model alone at a dose of 75 mg/kg maximally inhibited phosphorylation by IGF-IR (80%) between 4 and 24 hours, plasma drug concentrations ranged from 26.6 to 4.77 μm. OSI-906 at a dose of 60 mg/kg alone in NCI-H292 transplanted mice, 2,4,24 hours, inhibition of sugar absorption. OSI-906 in NCI-H292 transplantation mouse model, inhibit tumor growth. OSI-906 Inhibition of tumor growth in a IGF-IR-driven xenograft mouse model, treated at a dose of 75 mg/kg, resulting in 100% TGI and 55% regression, treated at a dose of 25 mg/kg, resulting in 60% TGI, there was no recession. Treatment of dogs, rats and mice OSI-906 induced different elimination half-lives of 1.18 hours, 2.64 hours and 2.14 hours, respectively. OSI-906 female Sprague-Dawley rats and female CD-1 mice were treated individually at different doses, once a day, and the V max value was not proportional to the OSI-906 dose. OSI-906 according to the dose of 25 mg/kg treatment for 12 days, improve the blood sugar value. OSI-906 treatment of a IGF-IR-driven human full-length human IGF-IR (LISN) transplanted mouse model alone at a dose of 75 mg/kg maximally inhibited phosphorylation by IGF-IR (80%) between 4 and 24 hours, plasma drug concentrations ranged from 26.6 to 4.77 μm. OSI-906 at a dose of 60 mg/kg alone in NCI-H292 transplanted mice, 2,4,24 hours, inhibition of sugar absorption. OSI-906 in NCI-H292 transplantation mouse model, inhibit tumor growth. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.372 ml | 11.862 ml | 23.724 ml |
5 mM | 0.474 ml | 2.372 ml | 4.745 ml |
10 mM | 0.237 ml | 1.186 ml | 2.372 ml |
5 mM | 0.047 ml | 0.237 ml | 0.474 ml |