1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. ARQ 069

ARQ 069 

Cat. No.: HY-101544
Handling Instructions

ARQ 069, an analog of ARQ 523, inhibits FGFR in an enantiospecific manner. ARQ 069 targets the unphosphorylated, inactive forms of FGFR1/FGFR2 kinases (IC50s of 0.84 μM and 1.23 μM, respectively). ARQ 069 inhibits FGFR1/FGFR2 autophosphorylation (IC50s of 2.8 and 1.9 μM, respectively) through a mechanism in a non-ATP competitive dependent manner.

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ARQ 069 Chemical Structure

ARQ 069 Chemical Structure

CAS No. : 1314021-57-2

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Description

ARQ 069, an analog of ARQ 523, inhibits FGFR in an enantiospecific manner. ARQ 069 targets the unphosphorylated, inactive forms of FGFR1/FGFR2 kinases (IC50s of 0.84 μM and 1.23 μM, respectively). ARQ 069 inhibits FGFR1/FGFR2 autophosphorylation (IC50s of 2.8 and 1.9 μM, respectively) through a mechanism in a non-ATP competitive dependent manner[1].

IC50 & Target[1]

unphosphorylated FGFR1

0.84 μM (IC50)

unphosphorylated FGFR2

1.23 μM (IC50)

FGFR1 autophosphorylation

2.8 μM (IC50)

FGFR2 autophosphorylation

1.9 μM (IC50)

In Vitro

ARQ 069 (3.8-60 μM; for 2 hours) reduces the degree of phosphorylation of FGFR (predominantly FGFR2) in a concentration-dependent manner, without decreasing β-actin[1].
ARQ 069 shows an affinity for FGFR2 of 5.2 μM[1].
ARQ 069 inhibits FGFR phosphorylation in Kato III cells with an IC50 of 9.7 μM[1].
ARQ 069 targets the inactive forms of FGFR1 and FGFR2 kinases and inhibits their enzymatic activity. When ARQ 069 is preincubated with either phosphorylated FGFR1 or FGFR2, the potency of ARQ 069 in inhibiting Pyk2 phosphorylation is markedly reduced, with IC50 values determined to be greater than 30 and 24.8 μM for FGFR1 and FGFR2, respectively. ARQ 069 exhibits at least a 20-fold preference for binding to the unphosphorylated, inactive forms of FGFR1 and FGFR2[1].
ARQ 068 is the R-enantiomer, and ARQ 069 is the S-enantiomer[1].

Western Blot Analysis[1]

Cell Line: Kato III human gastric carcinoma cells
Concentration: 3.8, 7.5, 15, 30, 60 μM
Incubation Time: For 2 hours
Result: Reduced the degree of phosphorylation of FGFR (predominantly FGFR2) in a concentration-dependent manner, without decreasing β-actin.
Molecular Weight

273.33

Formula

C₁₈H₁₅N₃

CAS No.

1314021-57-2

SMILES

NC1=NC=C2C[[email protected]@H](C3=CC=CC=C3)C4=CC=CC=C4C2=N1

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

ARQ 069ARQ069ARQ-069FGFRFibroblast growth factor receptoranalogARQ523enantioselectivelyunphosphorylatedFGFR1FGFR2autophosphorylationATPdependentInhibitorinhibitorinhibit

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