FLT3/CHK1-IN-2

Name: FLT3/CHK1-IN-2
Brand: TargetMol
SKU: T209231
Rating: 4.5 (1 reviews)

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Catalog No. T209231

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.

FLT3/CHK1-IN-2

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Catalog No. T209231

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Product Introduction

Bioactivity

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.

Chemical Properties

Formula

C₁₈H₂₃F₃N₆O₂S

Storage & Solubility Information

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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