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FIIN-2

Cat. No. M5127
FIIN-2 Structure
Size Price Availability Quantity
10mM*1mL in DMSO USD 155  USD155 In stock
5mg USD 110  USD110 In stock
10mg USD 175  USD175 In stock
25mg USD 350  USD350 In stock
50mg USD 580  USD580 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 634.73
Formula C35H38N8O4
CAS Number 1633044-56-0
Solubility (25°C) Water <1 mg/mL
DMSO 69 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Tan L,et.al. Proc Natl Acad Sci U S A. Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors.

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