1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
    FGFR
  3. FIIN-3

FIIN-3 

Cat. No.: HY-18603 Purity: 98.13%
Handling Instructions

FIIN-3 is an irreversible inhibitor of FGFR with an IC50 of 13.1, 21, 31.4, and 35.3 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.

For research use only. We do not sell to patients.

FIIN-3 Chemical Structure

FIIN-3 Chemical Structure

CAS No. : 1637735-84-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 402 In-stock
Estimated Time of Arrival: December 31
1 mg USD 108 In-stock
Estimated Time of Arrival: December 31
5 mg USD 264 In-stock
Estimated Time of Arrival: December 31
10 mg USD 420 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1440 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2220 In-stock
Estimated Time of Arrival: December 31
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Description

FIIN-3 is an irreversible inhibitor of FGFR with an IC50 of 13.1, 21, 31.4, and 35.3 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.

IC50 & Target[1]

FGFR1

13.1 nM (IC50)

FGFR2

21 nM (IC50)

FGFR3

31.4 nM (IC50)

FGFR4

35.3 nM (IC50)

In Vitro

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 good potency against gatekeeper mutant V564F; FIIN-3 also is potent against the gatekeeper-plus-1 mutant E565K; FIIN-3 also displays antiproliferative activity (with an EC50 of 135 nM) against Ba/F3 cells transformed by the EGFR vIII fusion protein, which has a WT EGFR kinase domain. 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[1].

Molecular Weight

691.61

Formula

C₃₄H₃₆Cl₂N₈O₄

CAS No.

1637735-84-2

SMILES

C=CC(NC1=CC=C(CN(C(NC2=C(Cl)C(OC)=CC(OC)=C2Cl)=O)C3=NC=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=C3)C=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (14.46 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4459 mL 7.2295 mL 14.4590 mL
5 mM 0.2892 mL 1.4459 mL 2.8918 mL
10 mM 0.1446 mL 0.7230 mL 1.4459 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

TEL-FGFR2–transformed Ba/F3 cells are seeded in a 96-well plate and are treated with each concentration of FIIN-3. After 72 h the cells are assessed by MTS tetrazolium assay[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 98.13%

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Keywords:

FIIN-3FIIN3FIIN 3EGFRFGFREpidermal growth factor receptorErbB-1HER1Fibroblast growth factor receptorInhibitorinhibitorinhibit

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FIIN-3
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HY-18603
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