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FLT3/CHK1-IN-1

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SI-7347

FLT3/CHK1-IN-1, >98% (HPLC)

CAS No. : [2991054-23-8]

IUPAC Name : 1-(6-((4-(((1s,4s)-4-Aminocyclohexyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)-3,4-dihydroisoquinolin-2(1H)-yl)-3-hydroxy-3-methylbutan-1-one

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5MGRequest A Quote
Back Order  Estimated to ship on 04 October 2026
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Chemical Properites
Mol. Formula :
C25H33F3N6O2
Mol. Weight :
506.57
Appearance :
Solid
Melting Point :
Not available
For Laboratory research use only, not for drug, household or other uses.

Applications : This is a dual FLT3/CHK1 inhibitor designed to overcome both acquired and adaptive resistance in FLT3‑mutant AML. It shows strong activity in BaF3 FLT3‑TKD and FLT3‑ITD/TKD resistance models, with >1700‑fold selectivity over c‑KIT and greatly reduced hERG affinity (IC50 = 58.4 μM), addressing a major cardiotoxicity liability of FLT3 inhibitors. Mechanistically, it upregulates p53 and suppresses the outgrowth of adaptive resistant cells. In vivo, it demonstrates favorable PK, good safety, robust tumor growth inhibition in MV‑4‑11 xenografts, and prolonged survival in Molm‑13 transplantation models, supporting its advancement as a next‑generation FLT3‑directed AML candidate.

References : Li X. et al.: J. Med. Chem., 66(17), 11792-11814, 2023.

Storage : Keep container tightly closed under nitrogen or argon and refrigerate for long-term shelf life.

Caution : In case of contact with skin or eyes, rinse immediately with plenty of water and seek medical advice. Wear suitable protective clothing and gloves.

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