egfr (t790m)

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.

PF-06459988 is a novel, effective, orally active, irreversible, and selective epidermal growth factor receptor (EGFR) mutant inhibitor. PF-06459988 has high efficiency and high affinity for EGFRs double mutants containing T790M, and has minimal activity against WT EGFR. PF-06459988 makes a candidate drug for the treatment of cancer.

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

EAI001 is a potent and selective mutant epidermal growth factor receptor (EGFR) variant inhibitor that inhibits EGFRL858R T790M with an IC50 value of 24 nM.EAI001 can be used in cancer research.

EGFR T790M L858R-IN-6 (compound 53), classified as a pyrimidine compound, serves as an effective inhibitor of EGFR T790M L858R, demonstrating 90.88% inhibition of enzyme activity at a concentration of 0.05 μM [1].

EGFR T790M L858R-IN-5 (example 52) functions as a potent EGFR T790M L858R inhibitor, demonstrating a 92.9% inhibition rate at a concentration of 0.05 μM [1].

EGFR T790M L858R-IN-7 (Compound 72), a novel pyrimidine compound, exhibits high efficacy in inhibiting the EGFR T790M and L858R mutations, with a 93% inhibition rate at 0.05 μM. It achieves its inhibitory action by specifically binding to the kinase domain of EGFR, which prevents phosphorylation activity [1].

EGFR T790M L858R-IN-4, a potent inhibitor of EGFR T790M L858R with anticancer properties (WO2024064091A1; Example 14) [1].

EGFRT790M L858R-IN-2 is a potent, selective inhibitor of EGFRT790M L858R, exhibiting IC50 values of 3.5 nM for EGFRT790M L858R and 1290 nM for EGFR WT. This compound effectively decreases the expression of p-EGFR, P-AKT, P-ERK1 2, and induces apoptosis as well as cell cycle arrest in the G1 phase, demonstrating anti-cancer activity [1].

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.

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.

Osimertinib (AZD-9291) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.

Wighteone (Erythrinin B) is a small molecule compound derived from Genista ephedroides with potential antifungal and anticancer activity against EGFR L858R T790M mutant non-small cell lung cancer.

EGFR-IN-9 is a potent EGFR kinase inhibitor with IC50s of 7 nM, 28 nM for the wild type EGFR kinase and double mutant EGFR kinase (L858R T790M). EGFR-IN-9 has antitumor activity.

DBPR112 is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM for EGFRWT and 48 nM for EGFRL858R T790M, capable of occupying the ATP-binding site and demonstrating significant antitumor efficacy.

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.

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.

BI-4732 is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with high blood-brain barrier permeability, antitumor activity, inhibition of EGFR activation, and inhibition of T790M mutations.

BI-4020 is a fourth-generation, orally active, and non-covalent inhibitor of EGFR tyrosine kinase. It exhibits activity against the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines), the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM), and EGFR wt (IC50=190 nM). BI-4020 also shows high kinome selectivity and good DMPK properties.

EGFR-IN-87 is a potent EGFR tyrosine kinase inhibitor with anticancer activity that inhibits EGFR_d746-750, EGFR_L858R T790M, and EGFR_WT in A431 cells, and can be used for cancer research.

Osimertinib mesylate (AZD-9291 mesylate) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib mesylate has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.

(S)-Afatinib (BIBW2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 0.4 10 14 1 nM for EGFRwt, EGFR (L858R), EGFR (L858R T790M), HER2, and HER4, respectively.

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.