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.
|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|
|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.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 50 mg/mL|
|Related VEGFR/PDGFR Products|
SU 5205 is a VEGFR2 inhibitor.
SU-5408 is a potent, cell-permeable inhibitor of mouse VEGFR2 kinase with IC50 of 70 nM.
BFH772 is a potent and selective VEGFR2 inhibitor with an IC50 value of 3 nM.
Ranibizumab is a monoclonal antibody that inhibits angiogenesis by inhibiting Vascular endothelial growth factor A.
NVP-ACC789 is an inhibitor of human VEGFR-1, VEGFR-2 (mouse VEGFR-2), VEGFR-3 and PDGFR-β with IC50s of 0.38, 0.02 (0.23), 0.18, 1.4 μM, respectively.
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