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FIIN-3

Cat. No. M8938
FIIN-3 Structure
Size Price Availability Quantity
5mg USD 280  USD280 In stock
10mg USD 450  USD450 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

FIIN-3 is the first inhibitor that can potently inhibit the proliferation of cells dependent upon the gatekeeper mutants of FGFR1 or FGFR2, which confer resistance to first-generation clinical FGFR inhibitors such as NVP-BGJ398 and AZD4547. FIIN-3 potently inhibits both WT FGFRs (EC50 in the 1- to 41-nM range) and the gatekeeper mutant of FGFR2 (EC50 of 64 nM). FIIN-3 also strongly inhibits EGFR, with an EC50 of 43 nM.

FIIN-3 shows even better activity against EGFR mutant L858R (EC50 of 17 nM) and moderate activity, displaying an EC50 of 231 nM, against the EGFR mutant L858R/T790M mutant. In WT FGFR2 Ba/F3 cells, FIIN-3 completely inhibits the FGFR2 autophosphorylation on Tyr656/657 at concentrations as low as 3 nM. In FGFR2 V564M Ba/F3 cells, FIIN-3 is capable of inhibiting the FGFR2 mutant V564M autophosphorylation with partial inhibition at 100 nM and complete inhibition observed at 300 nM.

Customer Product Validations & Biological Datas
Source Proc Natl Acad Sci U S A (2014 Nov). Figure 4. FIIN-3
Method Western blot
Cell Lines H1581 (FGFR1 WT or V561M) cells
Concentrations 1.0 µM
Incubation Time 12 h
Results The downstream prosurvival signaling pathways of FGFR also were examined in these cell lines, showing that FIIN-2, FIIN-3, and BGJ398 effectively suppressed p-FRS2, p-FGFR, p-AKT, and p-ERK in these FGFR-activated cells at 1.0 µM, except that BGJ398 failed in the FGFR1 V561M H1581 cells. In H1581 cells they also inhibited FGFR V561M in a dose-responsive manner, with both of them inhibiting most autophosphorylation of FGFR1 V561M at 333 nM, whereas BGJ398 still was inactive at 1.0 µM.
Protocol
Cell Experiment
Cell lines H1581 (FGFR1 WT or V561M) cells
Preparation method Inhibition of FGFR-dependent signaling by BGJ398, FIIN-2, and FIIN-3 in H1581 (FGFR1 WT or V561M) cells. Cells were treated with indicated inhibitors at 1.0 µM for 12 h and then were lysed and subjected to Western blot for the indicated proteins or phosphoproteins.
Concentrations 1.0 µM
Incubation time 12 h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 691.61
Formula C34H36Cl2N8O4
CAS Number 1637735-84-2
Purity >98%
Solubility DMSO: 10 mg/mL
Storage at -20°C
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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Keywords: FIIN-3 supplier, FGFR, inhibitors

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