1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. FIIN-1

FIIN-1  (Synonyms: FGFR irreversible inhibitor-1)

Cat. No.: HY-15813 Purity: 99.11%
COA Handling Instructions

FIIN-1 is a potent, irreversible, selective FGFR inhibitor. FIIN-1 binds to FGFR1/2/3/4 and Flt1/4 with Kds of 2.8/6.9/5.4/120 nM and 32/120 nM respectively. The biochemical IC50s of FIIN-1 are 9.2, 6.2, 11.9, and 189 nM against FGFR1/2/3/4, respectively.

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FIIN-1 화학구조

FIIN-1 화학구조

CAS No. : 1256152-35-8

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고객리뷰

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

FIIN-1 is a potent, irreversible, selective FGFR inhibitor. FIIN-1 binds to FGFR1/2/3/4 and Flt1/4 with Kds of 2.8/6.9/5.4/120 nM and 32/120 nM respectively. The biochemical IC50s of FIIN-1 are 9.2, 6.2, 11.9, and 189 nM against FGFR1/2/3/4, respectively[1].

IC50 & Target[1]

FGFR1

2.8 nM (Kd)

FGFR2

6.9 nM (Kd)

FGFR3

5.4 nM (Kd)

FGFR4

120 nM (Kd)

FGFR1

9.2 nM (IC50)

FGFR2

6.2 nM (IC50)

FGFR3

11.9 nM (IC50)

FGFR4

189 nM (IC50)

In Vitro

FIIN-1 binds to BLK, ERK5, KIT, MET, PDGFRB and VEGFR2 with Kds of 65 nM, 160, 420, 1000, 480 and 210 nM, respectively. The IC50s for Blk and Flt1 are 381 nM and 661 nM respectively[1].
FIIN-1 (14 nM-46 μM; 72 hours) inhibits proliferation of FGF signaling-sensitive cancer cell lines[1].
FIIN-1 (20 nM) inhibits iFGFR1 autophosphorylation and its downstream Erk1/2 almost completely.

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

Cell Proliferation Assay[1]

Cell Line: Stomach KATO III, SNU-16 and FU97 cells; Bladder RT4 cells; Kidney G-401 and G-402 cells; Lung SBC-3 and H520 cells; Pancreas A2.1 cells; Ovary A2780 and PA-1 cells; Bone RD-ES cells
Concentration:
Incubation Time: 72 hours
Result: The EC50 of 70 nM for Bladder RT4 cell.
The EC50 of 230 nM for Pancreas A2.1 cell.
The EC50 of 2.3 μM for Bone RD-ES cell.
EC50s of 0.22 and 4.6 μM for Ovary A2780 and PA-1 cells, respectively.
EC50s of 0.08 and 4.5 μM for Lung SBC-3 and H520 cells, respectively.
EC50s of 0.14 and 1.65 μM for Kidney G-401 and G-402 cells, respectively.
EC50s of 0.014, 0.03 and 0.65 μM for Stomach KATO III, SNU-16, FU97 cells, respectively.

Western Blot Analysis[1]

Cell Line: Serum-starved MCF10A cells that stably express iFGFR1
Concentration: 20 nM
Incubation Time: 30 minutes
Result: Blocked activation of iFGFR1 and phosphorylation of downstream effectors Erk1/2.
분자량

656.60

화학식

C32H39Cl2N7O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C=CC(NC1=CC=CC(CN(C2=NC(NCCCCN(CC)CC)=NC=C2CN3C4=C(Cl)C(OC)=CC(OC)=C4Cl)C3=O)=C1)=O

선적

Room temperature in continental US; may vary elsewhere.

보관
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
순도&문서
References
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FIIN-1 Related Classifications

  • 몰농도 계산기

  • 농도 희석 계산기

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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상품명:
FIIN-1
Cat. No.:
HY-15813
수량:
MCE Japan Authorized Agent: