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FLT3/CHK1-IN-2 (Compound 30) is a dual inhibitor targeting FLT3 and CHK1, with IC50 values of 25.63 nM for CHK1, 16.39 nM for FLT3-WT, and 22.80 nM for FLT-D835Y. It displays favorable oral pharmacokinetic properties and kinase selectivity. FLT3/CHK1-IN-2 is applicable in acute myeloid leukemia (AML) research.
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| Description | FLT3/CHK1-IN-2 (Compound 30) is a dual inhibitor targeting FLT3 and CHK1, with IC50 values of 25.63 nM for CHK1, 16.39 nM for FLT3-WT, and 22.80 nM for FLT-D835Y. It displays favorable oral pharmacokinetic properties and kinase selectivity. FLT3/CHK1-IN-2 is applicable in acute myeloid leukemia (AML) research. |
| In vitro | FLT3/CHK1-IN-2 exhibits antiproliferative effects on MV4-11 cells with an IC₅₀ of less than 4 nM. This compound also shows antiproliferative activity against BaF3 cells containing various FLT3 mutations, with IC₅₀ values for BaF3-FLT3-F691L, BaF3-FLT3-D835F, BaF3-FLT3-D835V, BaF3-FLT3-ITD, and BaF3-FLT3-ITD/D835Y being 28.96, 29.30, 26.37, 30.24, and 75.81 nM, respectively. Additionally, FLT3/CHK1-IN-2, within the concentration range of 0-100 nM, inhibits the phosphorylation of FLT3 and its main downstream effectors STAT5 (Tyr694), AKT (Ser473), and ERK (Tyr204) in MV4-11 cells, while also reducing pS296-CHK1 levels and c-Myc protein expression. |
| In vivo | FLT3/CHK1-IN-2 (20 mg/kg, oral administration) demonstrates favorable pharmacokinetic (PK) properties, with a maximum concentration (C max) of 2213.07 ng/mL and an area under the curve (AUC(0−t)) of 2736.58 h·ng/mL. |
| Formula | C18H23F3N6O2S |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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