EGFR-IN-1 TFA is an orally active and irreversibleL858R/T790M mutant selectiveEGFRinhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistantEGFRL858R, T790M with 100-fold selectivity over wild-typeEGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity^[1].

EGFR-IN-1 TFA (compound 24) is an orally active and irreversibleL858R/T790M mutant selective EGFRinhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity^[1].

EGFR-IN-1 TFA (30 mg/kg; p.o.; daily for 2 weeks) displays significant tumor growth inhibition with no observed loss in body weight^[1].
EGFR-IN-1 TFA evaluates in a time course PD experiment upon oral dosing at 30 mg/kg. EGFR-IN-1 TFA shows a >50% inhibition of phosphorylation of EGFR for >12 h. EGFR-IN-1 TFA reaches maximal concentration of 0.10 μM at 2 h and systemic exposure (AUC0-inf.) is 0.33 μM. h^[1].

628.60

Solid

C₃₀H₃₁F₃N₆O₆

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

DMSO : 250 mg/mL(397.71 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。