Regorafenib targets both tumor cell proliferation and tumor vasculature through inhibition of receptors of tyrosine kinases (VEGFR, KIT, RET, FGFR, and PDGFR) and serine/threonine kinases (Raf and p38MAPK).Regorafenib suppresses growth of human Hep3B, PLC/PRF/5 and HepG2 cells in a concentration- and time-dependent manner
|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||10 mM in ethanol|
Targeted therapy for metastatic renal cell carcinoma: current treatment and future directions.
Heng DY,et.al. Ther Adv Med Oncol. 2010 Jan;39-49. PMID: 21789125.
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|EG00229 Trifluoroacetate salt
EG00229 Trifluoroacetate is the first small molecule inhibitor of the neuropilin-1 and VEGF-A interaction with an IC50 of inhibition of 8 uM (125I-VEGF binding to PAE/NRP1 cells).
Apatinib is a selective VEGFR2 inhibitor with IC50 of 1 nM.
JI-101 is an orally available multi-kinase inhibitor of VEGFR2，PDGFRβ and EphB4 with potential antiangiogenic and antineoplastic activities.
BAW2881 (NVP-BAW2881) is a potent and selective VEGFR2 inhibitor with activity to inhibit chronic and acute skin inflammation.
SU 1498 is a selective inhibitor of the receptor tyrosine kinase VEGF receptor 2 (VEGFR2, aka FLK1; IC50 = 700 nM).
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