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Arg-IN-1 is a selective covalent inhibitor targeting Arginine (Arg), with IC50 values of 9.7 nM and 30.4 nM for FGFR2 and FGFR3, respectively. This compound is designed to potentially avoid the off-target toxicity of FGFR1/4 and overcome acquired resistance, offering potential in cancer therapies targeting FGFR.
Pack Size | Price | Availability | Quantity |
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10 mg | Inquiry | Backorder | |
50 mg | Inquiry | Backorder |
Description | Arg-IN-1 is a selective covalent inhibitor targeting Arginine (Arg), with IC50 values of 9.7 nM and 30.4 nM for FGFR2 and FGFR3, respectively. This compound is designed to potentially avoid the off-target toxicity of FGFR1/4 and overcome acquired resistance, offering potential in cancer therapies targeting FGFR. |
Targets&IC50 | FGFR2:9.7 nM |
In vitro | Arg-IN-1 (Compound RF3) exhibits remarkable selectivity for FGFR2 and FGFR3, with IC₅₀ values of 9.7 nM and 30.4 nM, respectively. Its inhibitory effect on FGFR1 and FGFR4 is significantly reduced by factors of 244 and 765 (IC₅₀: 2367.6 nM and 7418.4 nM). Additionally, Arg-IN-1 demonstrates excellent anti-resistant activity, with an IC₅₀ of 9.4 nM against the FGFR2 V564F mutation. |
Formula | C36H42N12O6 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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