In FGFR1-4 Ba/F3 cells, FIIN-2 inhibits cell proliferation with EC50 in the single- to double-digit nanomolar range. FIIN-2 also shows excellent antiproliferative activity in a variety of backgrounds, including cell lines that have gatekeeper mutations in FGFR1 and that are dependent on FGFR4.In a zebrafish developmental model, FIIN-2 causes mild or severe phenotypes to the tail morphogenesis by inhibiting FGFR.
|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||Water <1 mg/mL;DMSO 69 mg/mL|
Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors.
Tan L,et.al. Proc Natl Acad Sci U S A. 2014 Nov 11;E4869-77. PMID: 25349422.
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