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ZM 306416 is a VEGFR (Flt and KDR) inhibitor for VEGFR1 with IC50 of 0.33 μM, but also found to inhibit EGFR with IC50 of <10 nM.
| 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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
| Molecular Weight | 333.74 |
| Formula | C16H13ClFN3O2 |
| CAS Number | 690206-97-4 |
| Purity | >99% |
| Solubility | DMSO 50 mg/mL |
| Storage | at -20°C |
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Source | J Biomol Screen (2012). Figure 6. ZM 306416 |
| Method | Assessment of the anti-proliferative effects of hits against a panel of established cell lines | |
| Cell Lines | EGFR cell lines A549 and H2030 | |
| Concentrations | 10 μM | |
| Incubation Time | - | |
| Results | Confirming the newly identified inhibitory activity of ZM-306416 toward EGFR, this compound induced selective anti-proliferative effect toward the EGFR addicted NSCLC cell lines H3255 and HCC4011, while sparing the wild type EGFR cell lines A549 and H2030. | |
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