egfrt790m

CHMFL-EGFR-202 is a potent, irreversible inhibitor of EGFR mutant kinase with IC50 values of 5.3 nM for drug-resistant mutant EGFR T790M and 8.3 nM for WT EGFR kinases.

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.

AV-412 (MP412) is an EGFR inhibitor for EGFR, EGFR T790M, EGFR L858R, EGFR L858R/T790M, and ErbB2, with IC50 values of 0.75, 0.79, 0.5, 2.3, and 19 nM, respectively.

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

Rociletinib hydrobromide is an orally delivered inhibitor of the mutant form of EGFR kinase (Kis: 21.5 nM and 303.3 nM for EGFR L858R/T790M and EGFR WT).

Oritinib (SH-1028) is an inhibitor of EGFR with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM for EGFR (wt), EGFR (L858R), EGFR (L861Q), EGFR (L858R/T790M), EGFR (d746-750), EGFR (d746-750/T790M), respectively. Oritinib can be used in studies about the treatment of non-small cell lung cancer.

LSD1/EGFR-IN-1 (compound L-1) is an effective inhibitor of LSD1, EGFRT790M/L858R, and EGFRL858R/T790M/C797S, with IC50 values of 6.24, 2.06, and 5.01 μM, respectively. This compound plays a significant role in cancer research.

EGFRT790M/L858R-IN-9 (Compound 8) is an inhibitor targeting the EGFR-L858R/T790M mutations. It effectively inhibits the phosphorylation of the EGFR-L858R/T790M mutant kinase, demonstrating an IC50 value of 0.0064 µM. Additionally, EGFRT790M/L858R-IN-9 can suppress the proliferation of non-small cell lung cancer (NSCLC) cells, making it useful for cancer research.

Avitinib (Abivertinib) maleate dihydrate is a third-generation, irreversible, orally active selective EGFR inhibitor with IC50 values of 0.18 nM for EGFRL858R and EGFRT790M, and 7.68 nM for wild-type EGFR. Additionally, Avitinib maleate dihydrate functions as a BTK inhibitor, promoting apoptosis in mantle cell lymphoma cells and inhibiting BTK phosphorylation, demonstrating anticancer properties.

EGFR/COX-2-IN-1 is an EGFR/COX-2 inhibitor that effectively targets EGFRWT, EGFRT790M, COX-1, and COX-2 with IC50 values of 0.12, 0.076, 20.1, and 1.52 μM, respectively. It inhibits MCF-7, HT-29, and A-549 cells with IC50 values of 1.20, 5.14, and 14.81 μM, respectively. The compound induces apoptosis by upregulating Bax protein and downregulating Bcl-2 protein levels. Additionally, EGFR/COX-2-IN-1 significantly increases the proportion of cells in the G2/M phase in MCF-7 cells, demonstrating a broad-spectrum antitumor effect.

EGFR/VEGFR2-IN-5 (Compound 14) is an orally active dual inhibitor of EGFR and VEGFR2, exhibiting an IC50 value of 1.15 µM for VEGFR2 and 0.28 µM for EGFRT790M. This compound demonstrates significant anticancer activity.

EGFR-IN-160 is an EGFR inhibitor with IC50 values of 1.62, 0.49, and 0.98 μM for EGFRWT, EGFRT790M, and EGFRL858R/T790M/C797S, respectively. It can induce cell cycle arrest at the G2/M and S phases and apoptosis (Apoptosis) in NCI-H522 cells, demonstrating anticancer properties. Additionally, EGFR-IN-160 exhibits antioxidant activity against DPPH (IC50: 12.11 µM) and H2O2 (IC50: 8.89 µM).

EGFR-IN-156 (Compound 7f) is an EGFR inhibitor with inhibitory activity against mutant EGFRL858R and EGFRT790M, with IC50 values of 0.186, 0.131, and 0.107 μM, respectively. It exhibits significant anticancer activity against human cancer cell lines HepG-29 (liver cancer), MCF-7 (breast cancer), and HCT-116 (colon cancer), with IC50 values of 1.67, 5.32, and 6.56 μM, respectively. EGFR-IN-156 suppresses cancer cell proliferation by inducing cell cycle arrest at the G/G1 phase and triggering apoptosis. It shows potential in EGFR-related cancers.

EGFRT790M/L858R-IN-3 (compound B1) is an EGFRL858R/T790M inhibitor with an IC50 value of 13 nM. In H1975 cells, EGFRT790M/L858R-IN-3 demonstrates antitumor activity with an IC50 of 0.087 μΜ. Additionally, it inhibits cell migration in A549 cells and induces apoptosis in H1975 cells (cellapoptosis).

T-1-DOCA is an EGFR inhibitor with IC50 values of 56.94 nM for EGFRWT and 269.01 nM for EGFRT790M. It has the capability to induce apoptosis (cellapoptosis) in HCT-116 cells.

EGFRWT/T790M/L858R-IN-1 (compound 10d) is a potent inhibitor of EGFR, demonstrating IC50 values of 0.097, 0.280, and 0.051 μM for EGFRWT, EGFRT790M, and EGFRL858R, respectively. This compound can be utilized in cancer research.

EGFR-IN-96 (compound 7a) is a thiophene[2,3-d]pyrimidine EGFR inhibitor that can induce apoptosis. It causes HepG2 cells to arrest in the S and G2/M phases and inhibits the growth of cancer cells with wild-type EGFR and EGFRT790M.

EGFRT790M/L858R/ACK1-IN-1 (Compound 21a) is a dual inhibitor targeting EGFRT790M/L858R and ACK1 with IC50 values of 23 nM and 263 nM, respectively. This compound effectively inhibits cell proliferation and exhibits antitumor activity.

EGFRWT/T790M-IN-1 (Compound 16h) is a dual inhibitor targeting both EGFRWT and EGFRT790M. It can arrest the cell cycle at the G2/M phase and induce apoptosis. Additionally, EGFRWT/T790M-IN-1 exhibits anticancer activity.

EGFRWT/T790M-IN-2 (Compound 7c) is an inhibitor of EGFR T790M/WT with IC50 values of 0.08 and 0.13 μM, respectively. This compound induces apoptosis by arresting the cell cycle at the G0-G1 phase and demonstrates antitumor activity.

Mutant EGFR inhibitor is a selective and potent Mutated EGFR inhibitor, inhibits L858R activating mutant, the Exonl9 deletion activating mutant and the T790M resistance mutant.

WZ8040-hydroxyl is a derivative or analogue molecule of WZ8040 with an additional hydroxyl group on the benzene ring. It is a novel mutant selective irreversible EGFRT790M inhibitor with potential anticancer activity.

Limertinib (ASK120067) is an orally active and highly efficient epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor targeting EGFR T790M. Limertinib can be used for studying non-small cell lung cancer.

CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.