egfr-in-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-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.

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.

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.

Dual Galectin-3/EGFR-IN-1 (Compound 29) is a dual inhibitor targeting Galectin-3 and EGFR, with dissociation constants (KD) of 52.29 μM and 3.31 μM, respectively. It inhibits TGF-β-induced hepatic stellate cell (HSC) activation, induces apoptosis in LX-2 cells, and shows antifibrotic activity in the liver.

TrxR/EGFR-IN-1 (Compound L1Au2) is a TrxR/EGFR inhibitor with activity against both gefitinib-sensitive and -resistant lung cancer, effectively suppressing tumor proliferation and promoting apoptosis. It enhances GPX4 degradation through autophagosome-lysosome and proteasome pathways, leading to ferroptosis. Additionally, it induces endoplasmic reticulum stress and triggers immunogenic cell death, making it applicable for studies on gefitinib-resistant lung cancer.

TopoisomeraseII/EGFR-IN-1 is a dual inhibitor of topoisomerase II and EGFR, exhibiting strong cytotoxic activity against the MCF-7, A549, and HCT-116 cell lines. It also demonstrates significant apoptotic activity, making it useful for cancer research.

PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual inhibitor targeting PRMT5 and EGFR, with IC50 values of 15.47 μM and 19.31 μM, respectively. It demonstrates antiproliferative activity against the A549, MCF7, HeLa, and MDA-MB-231 cell lines. This compound also exhibits favorable pharmacokinetic (PK) and pharmacodynamic (PD) properties in vivo and significantly inhibits the growth of MCF7 orthotopic xenograft tumors.

SOS1/EGFR-IN-1 (compound SE-9) is a dual-target inhibitor for prostate cancer, effectively suppressing downstream effector molecules through the inhibition of SOS1 and EGFR. It induces apoptosis and G1 phase cell cycle arrest, reducing angiogenesis and migration. In prostate cancer cells PC-3, it demonstrates significant antitumor activity with an IC50 of 0.45±0.03 μM.

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] .

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].

GLUT1/EGFR-IN-1 (compound H) is a potent inhibitor of both GLUT1 and EGFR. It targets the ATP-binding site of the EGFR tyrosine kinase and inhibits GLUT1-mediated energy metabolism, resulting in reduced ATP, MMP, intracellular lactate, and nuclear translocation of EGFR. GLUT1/EGFR-IN-1 is applicable in the research of nasopharyngeal carcinoma (NPC) and triple-negative breast cancer (TNBC).

EGFR-IN-12 (EGFR Inhibitor) is a cell permeable and selective inhibitor of EGFR kinase (IC50: 21 nM) and blocks receptor autophosphorylation in cells.

EGFR-IN-16 (AG473) is an inhibitor of EGFR in human A431 cells.

EGFR-IN-101 (I-10), a 2-phenylamino pyrimidine derivative, is an EGFR inhibitor with IC50 values of 33.26 nM for EGFR L858R/T790M/C797S and 106.4 nM for Ba/F3-EGFR L858R/T790M/C797S. It is applicable in the study of non-small cell lung cancer (NSCLC) [1].

EGFR-IN-102 (compound 6), an orally active EGFR inhibitor, demonstrates an IC 50 of 2 nM and is utilized for research in non-small-cell lung cancer [1].

EGFR-IN-103 (compound 1), an effective EGFR inhibitor, exhibits a strong inhibitory activity with an IC50 value of 6 nM against pEGFR [1].

EGFR-IN-104 (Compound A23) acts as a potent EGFR inhibitor, demonstrating IC50 values of 0.33 μM for EGFR L858R/T790M and 0.133 μM for EGFR Del19/T790M/C797S. It exhibits anticancer properties, effective both in vitro and in vivo [1].

EGFR-IN-105 (Compound 5b), an EGFR2 inhibitor with an IC50 value of 0.68 μM, exhibits anticancer activity and induces apoptosis in cancer cells, making it valuable for pancreatic cancer research [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].

EGFR-IN-11 is a selective inhibitor of EGFR-tyrosine kinase and induces cell apoptosis. EGFR-IN-11 inhibits triple mutant EGFRL858R/T790M/C797S with an IC50 of 18 nM and arrests cell cycle at G0/G1.

EGFR-IN-127 is an ATP-competitive inhibitor targeting EGFR, with IC50 values of 136.3 nM for EGFRdel19 and 161.2 nM for EGFRdel19/T790M/C797S. This compound holds potential for the study of non-small cell lung cancer (NSCLC).

EGFR-IN-124 (compound 10A) is an EGFR inhibitor with an IC50 value of 0.54 μM, utilized in cancer research.

EGFR-IN-129 (Compound 10b) is an effective, selective EGFR inhibitor with an IC50 of 51.2 nM and demonstrates broad-spectrum antiproliferative activity against the NCI tumor panel.