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ACK1 inhibitor

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SI-7949

ACK1 inhibitor, >98% (HPLC)

IUPAC Name : (R)-N-(3-(2-((2-Ethoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-8-((tetrahydrofuran-2-yl)methyl)-7,8-dihydropyrido[2,3-d]pyrimidin-6-yl)phenyl)-3-(trifluoromethyl)benzamide

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5MGRequest A Quote
Back Order  Estimated to ship on 04 October 2026
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50MGRequest A Quote
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Back Order  Estimated to ship on 04 October 2026
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Chemical Properites
Mol. Formula :
C39H40F3N7O4
Mol. Weight :
727.79
Appearance :
Solid
Melting Point :
Not available
For Laboratory research use only, not for drug, household or other uses.

Applications : This is a highly potent and selective ACK1 inhibitor (IC50 = 2.1 nM). It shows excellent kinome selectivity, sparing SRC, and robustly suppresses ACK1 and downstream AKT signaling in ASK120067‑resistant NSCLC cells. The compound demonstrates strong synergy with ASK120067 in vitro and exhibits reasonable PK with ~20% oral bioavailability, making it a promising lead for overcoming EGFR‑TKI resistance in NSCLC.

References : Li Q. et al.: J. Med. Chem., 66(10), 6905-6921, 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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