CP-724714 is a potent and selective orally active HER-2 tyrosine kinase inhibitor under development for the treatment of advanced HER2-overexpressing cancers. CP-724714 has no appreciable activity toward EGFR (IC50 = 6400 nM) and is furthermore selective with respect to insulin receptor, IGF1R, PDGFRβ, VEGFR2, ABL, SRC and CDK.
| Cell Experiment | |
|---|---|
| Cell lines | ZR-75-30, HCC-1419, MDA-MB-175, BT-474, SKBR3, MDA-MB-361, UACC-812, T-47D, MDA-MB-453, MDA-MB-468, CAMA-1, MDA-MB-157, MCF-7, MDA-MB-435, ZR-75-1, BT-20, and MDA-MB-231cells line |
| Preparation method | Cell proliferation assays. Cells were seeded in duplicate at 5,000 to 10,000 per well in 24-well plates. The day after plating, CP-724,714 was added by titrating over six or more dilutions from 10 μmol/L down. Control wells without drug were seeded as well. Cells were grown for 6 to 7 days, at which time surviving cells were counted. After trypsinization, cells were placed in isotone solution and counted immediately using a Coulter Z2 particle counter (Beckman Coulter, Inc.). Growth inhibition was calculated [(1- experimental value / control value) × 100] for each concentration. Dose-response curves were repeated at least twice and averaged. IC50 values were calculated using Calcusyn Software (Biosoft). |
| Concentrations | 0~10 μ M |
| Incubation time | 6-7 days |
| Animal Experiment | |
|---|---|
| Animal models | Athymic female mice bearing human tumor cells (BT-474 and MDA-MB-453) xenograft models |
| Formulation | formulated in 0.5% methylcellulose |
| Dosages | 30 and 100mg/kg bid for 8-40 days |
| Administration | p.o. |
| Molecular Weight | 469.53 |
| Formula | C27H27N5O3 |
| CAS Number | 537705-08-1 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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