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EGFR mutant-IN-2

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SI-7958

EGFR mutant-IN-2, >98% (HPLC)

CAS No. : [2770009-06-6]

IUPAC Name : 1-(2-(Dimethylamino)ethyl)-N-(4-(1-(ethylsulfonyl)-1H-indol-3-yl)-5-(trifluoromethyl)pyrimidin-2-yl)-1H-indol-5-amine

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Chemical Properites
Mol. Formula :
C27H27F3N6O2S
Mol. Weight :
556.61
Appearance :
Solid
Melting Point :
Not available
For Laboratory research use only, not for drug, household or other uses.

Applications : This is a rationally designed fourth‑generation EGFR inhibitor developed to overcome Osimertinib resistance driven by the EGFR‑C797S mutation. It potently inhibits EGFR^L858R/T790M/C797S (IC50 = 14 nM) and suppresses proliferation of H1975‑TM cells with matching potency, showing >500‑fold selectivity over wild‑type EGFR. It also blocks EGFR^del19/T790M/C797S and inhibits PC9‑TM cell growth (IC50= 62 and 82 nM). The compound demonstrates favorable in vivo druggability, including solid PK, good safety, stability, and clear antitumor activity, positioning it as a promising fourth‑generation EGFR‑TKI lead for Osimertinib‑resistant NSCLC.

References : Dong H. et al.: J. Med. Chem., 66(10), 6849-6868, 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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