Pazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively.
|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||17 mg/mL in DMSO|
Pazopanib versus sunitinib in metastatic renal-cell carcinoma.
Motzer RJ, et al. N Engl J Med. 2013 Aug 22;369(8):722-31. PMID: 23964934.
|Related VEGFR/PDGFR Products|
ODM-203 is an orally available inhibitor of VEGFR and FGFR, with IC50s of 26, 9, 5 nM for VEGFR1, VEGFR2 and VEGFR3, and 11, 16, 6, 35 nM for recombinant FGFR1, FGFR2, FGFR3 and FGFR4, respectively.
MAZ51 is originally synthesized inhibitor of VEGFR-3 (Flt-4) tyrosine kinase, inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2.
SU14813 is a novel multiple receptor tyrosine kinase inhibitor with IC50s of 2, 50, 4, 15 nM for VEGFR-1, VEGFR-2, PDGFR-β and KIT.
SU 5205 is a VEGFR2 inhibitor.
SU-5408 is a potent, cell-permeable inhibitor of mouse VEGFR2 kinase with IC50 of 70 nM.
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