mutated egfr-in-1

Mutated EGFR-IN-1 (Osimertinib analog) is a valuable intermediate in designing inhibitors for mutated EGFR, including L858R EGFR, Exon19 deletion activating mutant, and T790M resistance mutant.

EGFR-IN-1 hydrochloride is an irreversible and specific inhibitor of L858R T790M mutant EGFR, with 100-fold selectivity over wild-type EGFR. It exhibits potent antitumor and antiproliferative activity in H1975 cells and mutant HCC827 cells with IC50s of 4 and 28 nM, respectively.

EGFR ErbB-2 inhibitor-1 is a selective ErbB2 HER2 inhibitor that effectively blocks ErbB2 and HER2 signaling.

EGFR/BRAF-IN-1, a 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivative, is a potent inhibitor of EGFR/BRAF, inhibiting BRAFV600E (IC50:45 nM) and cancer cell proliferation (GI50=35 nM), with good antioxidant effect.

EGFR BRAFV600E-IN-1 (Compound 23) is a potent dual inhibitor of EGFR (IC50: 0.08 μM) and BRAFV600E (IC50: 0.15 μM), exhibiting anti-proliferative effects on A-549 (IC50: 1.2 μM), MCF-7 (IC50: 0.79 μM), Panc-1 (IC50: 1.3 μM), and HT-29 (IC50: 1.23 μM).

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. )

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

EGFR kinase inhibitor 1 is a potent inhibitor of EGFR that acts on WT (IC50: 37 nM), l885R T790M (IC50: 1.7 nM), and L858R T790M C797S (IC50>300 nM). It is capable of blocking the cell cycle in G0 G1 phase, inducing apoptosis, and has an inhibitory effect on cell metastasis. Additionally, EGFR kinase inhibitor 1 exhibits anti-proliferative and anti-tumor effects.

ALK EGFR-IN-1 (Compound 8l) is a dual inhibitor targeting both ALK and EGFR, effectively blocking their phosphorylation. It demonstrates potent inhibition of ALK EGFR mutants with IC50 values of 4.3 nM for EGFR L858R T790M in H1975 cells and 3.6 nM for EML4-ALK in BaF3 cells. This compound may be applicable in the research of non-small cell lung cancer (NSCLC) [1].

EGFR C797S-IN-1 is a potent inhibitor targeting the EGFR-C797S mutation, with an IC50 value of 0.128 µM, exhibiting significant anti-proliferative and anti-tumor effects by inhibiting p-EGFR expression in a dose-dependent manner.

EGFR/CDK2-IN-1, an inhibitor of both EGFR and CDK2, demonstrates effective cytotoxicity towards MCF7 and HepG2 cells, suggesting its potential application in cancer research.

PROTAC PARP EGFR ligand 1 is a potent compound used in developing dual PARP-EGFR degraders via Proteolytic Targeting Chimera (PROTAC) technology [1].

EGFR/HER2/TS-IN-1 are EGFR, HER2 and TS (Thymidylate synthase) inhibitors with IC50 values of 0.203, 0.088 and 0.168 μM, respectively, and have the ability to induce apoptosis (MCF7 cell death).

EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. 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, an orally active and irreversible selective inhibitor targeting L858R/T790M mutant EGFR, exhibits strong antiproliferative and antitumor activity, particularly against H1975 cells and first line mutant HCC827 cells. This compound potently inhibits Gefitinib-resistant EGFR L858R/T790M mutations with a 100-fold selectivity over the wild-type EGFR.

EGFR HER2 DHFR-IN-1 is a highly selective and potent anticancer compound targeting MCF-7 breast cancer cells, acting as a multi-inhibitor for EGFR HER2 kinase and DHFR enzymes, with IC50 values of 0.153 μM, 0.108 μM, and 0.291 μM, respectively. It induces cell cycle arrest at the G1 S phase and apoptosis in cells [1].

EGFR CSC-IN-1 is a dual inhibitor of the epidermal growth factor receptor (EGFR [IC50 10.52 nM]) and cancer stem cells (CSC), potentially applicable in triple-negative breast cancer research.

EGFR HER2 CDK9-IN-1 (Compound 4) is a potent inhibitor of EGFR, HER2, and CDK9, with IC50 values of 90.17 nM, 131.39 nM, and 67.04 nM, respectively, and exhibits significant anti-tumor effects.

EGFR mutant- in-1, A 5-methylpyrimidopyridone derivative are effective selective EGFRL858R/T790M/C797S mutant inhibitors with IC50 of 27.5 nM, which significantly weakened EGFRWT effect.

MAPK-IN-2 (compound 3h) is an efficacious MAPK inhibitor with antineoplastic properties that significantly hinders proliferation across various cancer cell lines. It demonstrates robust suppression of the MAPK pathway (EGFR WT IC50 = 281 nM, c-MET IC50 = 205 nM, B-RAF WT IC50 = 112 nM, CDK4 6 IC50 = 95 and 184 nM, respectively) and exhibits pronounced activity against mutated forms of EGFR and B-RAF (EGFR T790M IC50 = 69 nM and B-RAF V600E IC50 = 83 nM) [1].