ARQ 069
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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- CAS No.: 1314021-57-2
- Formule: C18H15N3
- Masse moléculaire:273.33
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
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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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:Kato III human gastric carcinoma cells
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Concentration:3.8, 7.5, 15, 30, 60 μM
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Incubation Time:For 2 hours
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Result:Reduced the degree of phosphorylation of FGFR (predominantly FGFR2) in a concentration-dependent manner, without decreasing β-actin.
Chemical Information
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CAS No. 1314021-57-2
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Masse moléculaire 273.33
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Formule C18H15N3
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SMILES
NC1=NC=C2C[C@@H](C3=CC=CC=C3)C4=CC=CC=C4C2=N1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ARQ 069 Related Classifications
HY-101544 Related Classifications
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