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ARQ 069
Catalog No. T10372Cas No. 1314021-57-2
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. ARQ 069 shows an affinity for FGFR2 of 5.2 μM. ARQ 069 inhibits FGFR phosphorylation in Kato III cells (IC50: 9.7 μM). 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.
ARQ 069
Catalog No. T10372Cas No. 1314021-57-2
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. ARQ 069 shows an affinity for FGFR2 of 5.2 μM. ARQ 069 inhibits FGFR phosphorylation in Kato III cells (IC50: 9.7 μM). 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.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 25 mg | $1,520 | 6-8 weeks | |
| 50 mg | $1,980 | 6-8 weeks | |
| 100 mg | $2,500 | 6-8 weeks |
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Product Introduction
Bioactivity
Chemical Properties
| Description | 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. ARQ 069 shows an affinity for FGFR2 of 5.2 μM. ARQ 069 inhibits FGFR phosphorylation in K |
| Targets&IC50 | FGFR2 unphosphorylated:1.23 μM, FGFR2 autophosphorylation:1.9 μM, FGFR1 autophosphorylation:2.8 μM, FGFR1 unphosphorylated:0.84 μM |
| In vitro | ARQ 069 (3.8-60 μM; for 2 hours) reduces the phosphorylation of FGFR, predominantly FGFR2, in a concentration-dependent manner without affecting β-actin[1]. It exhibits an affinity for FGFR2 at 5.2 μM[1] and 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, inhibiting their enzymatic activity. Preincubation with phosphorylated FGFR1 or FGFR2 significantly reduces ARQ 069's potency in inhibiting Pyk2 phosphorylation, with IC50 values over 30 μM for FGFR1 and 24.8 μM for FGFR2. ARQ 069 shows a 20-fold preference for binding to unphosphorylated, inactive FGFR1 and FGFR2[1]. ARQ 068 is the R-enantiomer, while ARQ 069 is the S-enantiomer[1]. |
| Molecular Weight | 273.33 |
| Formula | C18H15N3 |
| Cas No. | 1314021-57-2 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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