FLT3/CHK1-IN-2 

FLT3/CHK1-IN-2 (Compound 30) is a dual inhibitor of FLT3 and CHK1, with IC₅₀s of 25.63, 16.39, 22.80 nM for CHK1, FLT3-WT, and FLT-D835Y respectively. FLT3/CHK1-IN-2 has favorable oral PK properties and kinase selectivity. FLT3/CHK1-IN-2 can be used for research of acute myeloid leukemia (AML)^[1].

FLT3/CHK1-IN-2 shows antiproliferation activity against MV4-11 cell (IC₅₀: <4 nM)^[1].
FLT3/CHK1-IN-2 shows antiproliferative activity against BaF3 cells with a variety of FLT3 mutations (IC₅₀: 28.96, 29.30, 26.37, 30.24, 75.81 nM for BaF3-FLT3-F691L, BaF3-FLT3-D835F, BaF3-FLT3-D835V, BaF3-FLT3-ITD, BaF3-FLT3-ITD/D835Y cells)^[1].
FLT3/CHK1-IN-2 (0-100 nM) inhibits the phosphorylation of FLT3 and its main downstream effectors, STAT5 (Tyr694), AKT (Ser473) and ERK (Tyr204) in MV4-11 cells, and decreases the pS296-CHK1 level and the c-Myc protein expression level^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

FLT3/CHK1-IN-2 (20 mg/kg, p.o.) has favorable PK properties, with the C_max of 2213.07 ng/mL, and the AUC(0−t) of 2736.58 h·ng/mL^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

444.47

C₁₈H₂₃F₃N₆O₂S

NCCCNC1=NC(NC2=CC(CCN(S(=O)(C)=O)C3)=C3C=C2)=NC=C1C(F)(F)F

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Deng M, et al. Discovery of 5-trifluoromethyl-2-aminopyrimidine derivatives as potent dual inhibitors of FLT3 and CHK1. RSC Med Chem. 2023 Dec 7;15(2):539-552.  [Content Brief]