egfrt790m

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.

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.

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.

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).

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.

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.

pan-HER-IN-1 (Compound C5) is an irreversible, orally active Pan-HER inhibitor that exhibits IC50 values of 0.38 nM for EGFR, 1.6 nM for HER4, 2.2 nM for EGFR T790M L858R, and 3.5 nM for HER2, respectively. pan-HER-IN-1 induces apoptosis and demonstrates antitumor activities.

EGFR-IN-49 is a potent and selective EGFR inhibitor that targets EGFRT790M (IC50: 65.0 nM) and EGFRT790M L858R (IC50: 13.6 nM), inducing apoptosis in a dose-dependent manner.

EGFR-IN-56 (Compound 13a) is a potent inhibitor of EGFR, targeting EGFRT790M (IC50: 541.7 nM) and EGFRT790M L858R (IC50: 132.1 nM), blocking the G2 M phase of the cancer cell cycle and inducing apoptosis.

pan-HER-IN-2 (Compound C6) is an orally active, reversible, broad-spectrum HER inhibitor that targets EGFR (IC50: 0.72 nM), HER4 (IC50: 2.0 nM), EGFRT790M (IC50: 8.2 nM), and L858R (IC50: 75.1 nM). pan-HER-IN-2 induces apoptosis and possesses anti-tumor effects.

EGFR-IN-60 is an effective, orally active, safe antitumor agent. EGFR-IN-60 significantly inhibits EGFRWT (IC50: 83 nM), EGFRT790M (IC50: 26 nM), EGFRL858R (IC50: 53 nM) and JAK3 (IC50: 69 nM). IN-60 inhibited H1975 cells carrying the EGFRT790M mutation (IC50: 1.32 μM) and A431 cells overexpressing EGFRWT (IC50: 4.96 μM). EGFR-IN-60 increased the Bax Bcl-2 ratio, which induced apoptosis induction and cell death.

WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).

EAI045, an allosteric inhibitor, targets towards drug-resistant EGFR mutants but avoids the wild-type receptor.

Theliatinib (Xiliertinib) tartrate is a potent and highly selective EGFR inhibitor with ATP-competitive and orally active properties, showing a K_i of 0.05 nM and an IC_50 of 3 nM for EGFR, and an IC_50 of 22 nM for the EGFR T790M L858R mutant, with over 50-fold selectivity for EGFR compared to other kinases.

EGFR-IN-75, an inhibitor of both EGFR WT and EGFR T790M, exhibits anticancer and antioxidant properties with IC50 values of 0.28 μM and 5.02 μM, respectively.