egfr wt/t790m-in-1

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/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.

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 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.

EGFR-IN-30, a potent inhibitor of EGFR, exhibits IC50 values of 1-10 nM and <1 nM for EGFR (WT) and EGFR (L858R/T790M/C797S), respectively. This compound is of potential interest for research into diseases characterized by cell proliferation, such as cancer.

EGFR-IN-61 (compound 22a), a potent EGFR kinase inhibitor, exhibits IC50 values of 42 nM for L858R/T790M, 137 nM for L858R/T790M/C797S, and 743 nM for WT. Additionally, it demonstrates antiproliferative activity against the A549 and H1975 cell lines, with IC50 values of 2.14 μM and 1.82 μM, respectively [1].

EGFR-IN-81 (Compound 10i), an EGFR inhibitor, demonstrates potent activity by inhibiting EGFR WT and the L858R/T790M mutation at IC50 values of 4.38 nM and 5.69 nM, respectively. It also exhibits cytotoxic effects against MCF-7 and HCT116 cell lines with IC50 values of 2.07 μM and 6.72 μM, respectively [1].

Antiproliferative Agent-34 (Compound A14), a multitarget kinase inhibitor, demonstrates IC50 values of 177 nM for EGFR L858R/T790M and 1567 nM for EGFR WT. Additionally, it inhibits JAK2, ROS1, FLT3, FLT4, and PDGFRα with respective IC50s of 30.93 nM, 106.90 nM, 108.00 nM, 226.60 nM, and 42.53 nM. In normoxic conditions, it suppresses the proliferation of H1975 and HCC827 cells with IC50 values below 40 nM, while under hypoxic conditions, its potency increases 4-6 fold, yielding IC50 values less than 10 nM [1].

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].

EGFR-IN-109 (compound 4), an EGFR inhibitor, displays IC 50 values of 25.8 nM for EGFR WT and 182.3 nM for EGFR T790M. This compound halts the growth of cancer cells at the G2/M phase and triggers both early and late apoptosis. It is applicable in cancer research [1].