mutated egfr in 3

Mutated EGFR-IN-3 is a ATP-competitive and highly selective allosteric dibenzodiazepinone EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) inhibitor(IC50 of 12 nM and 13 nM, respectively. )

EGFR-IN-3 is an EGFR inhibitor with potential antitumour activity.EGFR-IN-3 inhibits EGFRwt-TK and induces apoptosis (cell death), which can cause cells to block in the G2/M phase.

PROTAC EGFR Degrader 3, a highly potent molecule, exhibits remarkable cellular activity against H1975 and HCC827 cells, maintaining high selectivity. It additionally reveals the lysosome's crucial role in the degradation mechanism of mutant EGFR [1].

EGFR/HER2/DHFR-IN-3 (compound 4c) serves as an efficacious dual inhibitor specifically targeting EGFR/HER2, exhibiting IC50 values of 0.138 μM for EGFR and 0.092 μM for HER2, respectively. Moreover, it demonstrates inhibition of DHFR with an IC50 of 0.193 μM. Notably, this compound induces cell cycle arrest in the S phase and triggers apoptosis in MCF7 breast cancer cells [1].

Mutated EGFR-IN-2 is an inhibitor of mutant-selective EGFR.

EGFR/BRAFV600E-IN-3 is an inhibitor targeting EGFR, BRAFV600E, and EGFRT790M with IC50 values of 57 nM, 68 nM, and 9.70 nM, respectively. It induces apoptosis and exhibits promising antioxidant activity [1].

ALK/EGFR-IN-3 is a dual ALK and EGFR inhibitor that demonstrates potent anti-proliferative effects on various cancer cell lines, including H1975, PC9, and Baf3-EML4-ALK, with respective IC50 values of 0.1360, 0.0332, and 0.0339 μM [1].

EGFR/CDK2-IN-3 (compound 4b) serves as a dual inhibitor targeting both EGFR and CDK-2, exhibiting IC50 values of 71.7 nM and 113.7 nM, respectively. It prompts apoptosis in MCF-7 cells and halts the cell cycle in the S phase while demonstrating substantial anti-cancer cell toxicity, inhibiting MCF-7 cells with an IC50 of 3.16 μM [1].

Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant, and T790M resistance mutant.

EGFR/HER2/CDK9-IN-3 (Compound 10) is a potent inhibitor of EGFR (IC50:191.08 nM), HER2 (IC50:132.65 nM), and CDK9 (IC50:113.98 nM). EGFR/HER2/CDK9-IN-3 showed significant anti-tumor effects.

EGFR/HER2-IN-3 (Compound ZINC21942954) is a dual EGFR and HER2 inhibitor.