1. Protein Tyrosine Kinase/RTK
  2. FGFR

FIIN-2 

Cat. No.: HY-18602 Purity: 99.89%
Handling Instructions

FIIN-2 is an irreversible inhibitor of FGFR with an IC50 of 3.1, 4.3, 27, and 45 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.

For research use only. We do not sell to patients.
FIIN-2 Chemical Structure

FIIN-2 Chemical Structure

CAS No. : 1633044-56-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 170 In-stock
5 mg USD 122 In-stock
10 mg USD 192 In-stock
25 mg USD 384 In-stock
50 mg USD 660 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

FIIN-2 is an irreversible inhibitor of FGFR with an IC50 of 3.1, 4.3, 27, and 45 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.

IC50 & Target

IC50: 3.1 nM (FGFR1), 4.3 nM (FGFR2), 27 nM (FGFR3), 45 nM (FGFR4)[1]

In Vitro

FIIN-2 potently inhibits WT FGFRs (EC50s in the 1- to 93-nM range) and the gatekeeper mutant of FGFR2 (EC50 of 58 nM). FIIN-2 also moderately inhibits EGFR, with an IC50 of 204 nM. FIIN-2 inhibits proliferation of FGFR1-4 Ba/F3 cells with EC50s in the single- to double-digit nanomolar range and are especially potent against FGFR2, with EC50s in the 1-nM range. FIIN-2 shows good potency against gatekeeper mutant V564F[1].

In Vivo

Treatment of fish in the embryonic state with either FIIN-2 causes defects to the posterior mesoderm similar to the phenotypes reported following genetic knockdown of FGFR or treatment with other reported FGFR inhibitors. FIIN-2 causes mild or severe phenotypes to the tail morphogenesis in all treated embryonic zebrafish[1].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.5755 mL 7.8774 mL 15.7547 mL
5 mM 0.3151 mL 1.5755 mL 3.1509 mL
10 mM 0.1575 mL 0.7877 mL 1.5755 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

TEL-FGFR2–transformed Ba/F3 cells are seeded in a 96-well plate and are treated with each concentration of the compounds. 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
Molecular Weight

634.73

Formula

C₃₅H₃₈N₈O₄

CAS No.

1633044-56-0

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 30 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
FIIN-2
Cat. No.:
HY-18602
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