FLT3/CHK1-IN-1

• CAT Number: I040297
• CAS Number: 2991054-23-8
• Molecular Formula: C25H33F3N6O2
• Molecular Weight: 506.56
• Purity: ≥95%
• Synonyms: 1-[6-[[4-[(4-aminocyclohexyl)amino]-5-(trifluoromethyl)pyrimidin-2-yl]amino]-3,4-dihydro-1H-isoquinolin-2-yl]-3-hydroxy-3-methylbutan-1-one
• InChI: InChI=1S/C25H33F3N6O2/c1-24(2,36)12-21(35)34-10-9-15-11-19(6-3-16(15)14-34)32-23-30-13-20(25(26,27)28)22(33-23)31-18-7-4-17(29)5-8-18/h3,6,11,13,17-18,36H,4-5,7-10,12,14,29H2,1-2H3,(H2,30,31,32,33)
• InChIKey: LHDKPFSHXFFALR-UHFFFAOYSA-N
• SMILES: CC(C)(CC(=O)N1CCC2=C(C1)C=CC(=C2)NC3=NC=C(C(=N3)NC4CCC(CC4)N)C(F)(F)F)O

FLT3/CHK-IN-1 (CAT: I040297) is a potent dual inhibitor targeting FLT3 and CHK1 kinases, key regulators of oncogenic signaling and DNA damage response pathways. This compound exhibits over 1700-fold selectivity for FLT3 over c-KIT, minimizing off-target effects, and significantly reduces hERG channel affinity with an IC₅₀ of 58.4 μM, supporting an improved cardiac safety profile. FLT3/CHK-IN-1 demonstrates strong antitumor efficacy in vivo, effectively inhibiting tumor growth in mouse xenograft models using MV-4-11 leukemia cells. It is a valuable tool for preclinical research in acute myeloid leukemia (AML) and combination therapies targeting proliferative and checkpoint mechanisms.

Reference

FLT3/CHK-IN-1 (Compound 18) is a potent dual inhibitor targeting FLT3 and CHK1 kinases, key regulators of oncogenic signaling and DNA damage response pathways. This compound exhibits over 1700-fold selectivity for FLT3 over c-KIT, minimizing off-target effects, and significantly reduces hERG channel affinity with an IC₅₀ of 58.4 μM, supporting an improved cardiac safety profile. FLT3/CHK-IN-1 demonstrates strong antitumor efficacy in vivo, effectively inhibiting tumor growth in mouse xenograft models using MV-4-11 leukemia cells. It is a valuable tool for preclinical research in acute myeloid leukemia (AML) and combination therapies targeting proliferative and checkpoint mechanisms.