Molecular Formula | C18H13BrN4O
|
Molar Mass | 381.23 |
Density | 1.577±0.06 g/cm3(Predicted) |
Melting Point | 276 °C |
Solubility | DMSO: 13.67 mg/mL |
Appearance | Off-white to yellow solid. |
pKa | 9.84±0.43(Predicted) |
Storage Condition | Sealed in dry,Store in freezer, under -20°C |
In vitro study | CL-387785 blocks EGF-mediated receptor autophosphorylation in cells with an IC50 value of 5 nM. Of the cell lines that overexpressed EGF-R or c-erbB-2, CL-387785 inhibited cell proliferation predominantly as a cytostatic with an IC50 value of 31 nM. |
In vivo study | In nude mice overexpressing EGF-R, CL-387785(80 mg/kg/day, P. O.) effectively inhibited tumor growth. In the autosomal recessive polycystic kidney disease mouse model (ARPKD), Balb/EKI-785/bpk (BPK) mice were treated with c-bpk (90 mg/kg, I. P.), can significantly reduce the collection of tubular cystic lesions, improve renal function, reduce bile duct epithelial cell abnormalities, prolong survival. The EKI-785 dose as low as 25 mg/kg was able to reduce the xenograft tumor growth induced by HCA-7, and the dose of 100 mg/kg completely inhibited tumor growth. CL-387785 at 50 mg/kg was effective in inhibiting HCT-116 of the induced xenograft growth. |