egfr-in-7

EGFR-IN-7 (TQB3804) is a selective and potent EGFR kinase inhibitor.

VEGFR-IN-7 (Compound 2) is a VEGFR inhibitor that exhibits a modest inhibitory effect on angiogenesis. It holds potential for cardiovascular disease research.

EGFR-IN-71 is a potent inhibitor of epidermal growth factor receptor (EGFR) with an IC50 of 3.7 μM, and it has research value in chordoma.

EGFR-IN-70 is a potent EGFR inhibitor with IC 50 values of 23.6 and 307.5 nM for EGFR LR/TM/CS and EGFR WT , respectively. EGFR-IN-70 has anti-proliferative activity and suppresses phosphorylation of the EGFR . EGFR-IN-70 can be used for cancer research .

EGFR-IN-73 (Compound 3f) effectively inhibits the prevalent EGFR mutation, EGFR Del19, with an IC50 value of 119 nM [1].

EGFR-IN-74 is a potent inhibitor targeting EGFR, specifically effective against the L858R/T790M mutations, exhibiting an IC50 value of 138 nM. It effectively induces apoptosis in cancer cells.

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.

EGFR-IN-76 is a potent EGFR inhibitor.

EGFR-IN-78 (compound A5), a 2-aminopyrimidine derivative, serves as a reversible EGFR C797S-TK inhibitor and an apoptosis inducer. It exhibits anti-proliferative properties, impedes EGFR phosphorylation, and induces G2/M phase cell cycle arrest [1].

EGFR-IN-79 (compound 21), an EGFR inhibitor, exhibits antitumor activity through ROS-independent apoptosis and EGFR/AKT/mTOR-mediated autophagy. It effectively induces cell death in proliferating and quiescent zones of EJ28 spheroids and demonstrates a safety profile in zebrafish-based models [1].

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.

EGFR-IN-137 (Compound 4c) acts as an inhibitor of aromatase and EGFR, with IC50 values of 1.67 μg/mL and 0.08 μg/mL, respectively. It hinders the proliferation of cancer cells MCF-7 and MDA-MB-231, with IC50 values of 1.62 µM and 4.14 µM. Additionally, EGFR-IN-137 induces cell cycle arrest at the G0/G1 phase in MDA-MB-231 cells and triggers apoptosis through a caspase-dependent pathway.

EGFR-IN-142 (compound 9a) is an EGFR inhibitor with an IC50 value of 0.08 μM. It exhibits antiproliferative activity against MCF-7 cells (IC50 = 3.31 μM) and WI-38 cells (IC50 = 43.99 μM).

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-IN-159 (compound 12) is a dihydropyrimidine and a potent EGFR inhibitor with an IC50 of 29.00 nM. It exhibits dose-dependent inhibition of EGFR and HER2. The compound shows cytotoxicity against MCF-7 breast cancer cells and Vero cells with IC50 values of 16.07 μg/mL and 35.98 μg/mL, respectively. EGFR-IN-159 does not cross the blood-brain barrier (BBB) and demonstrates significant anticancer activity.

(3S)-Tanzisertib (hydrochloride) ((3S)-CC-930 (hydrochloride)) is an orally active JNK inhibitor, exhibiting IC50 values of 61 nM for JNK1, 7 nM for JNK2, and 6 nM for JNK3. It selectively inhibits ERK1, p38α, and EGFR, with IC50 values of 0.48 μM, 3.4 μM, and 0.38 μM, respectively. In an acute rat PK-PD model, (3S)-Tanzisertib (hydrochloride) suppresses LPS-induced TNFα production and is utilized in research on idiopathic pulmonary fibrosis (IPF).

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.

EGFR kinase inhibitor 2 (compound A-7) is a potent EGFR inhibitor targeting the mutations EGFRL858R/T790M/C797S and EGFRDel19/T790M/C797S. This compound shows potential in addressing acquired resistance in the treatment of non-small cell 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.

EGFR-IN-100 (compound 3f) is an EGFR inhibitor with an IC50 range of 0.137-0.507 μM. It exhibits antiproliferative activity and induces apoptosis. Additionally, EGFR-IN-100 arrests the cell cycle of MCF-7 cells at the S phase.

7-Bromoheptanoyl chloride is the link (ligand) in the formation of PROTACEGFR degrader 9.

EGFR-IN-118 (Compound 4a) is an inhibitor of the tyrosine kinase EGFR. It exhibits anticancer properties, effectively inhibiting the proliferation of MCF-7 and PC3 cells, with IC50 values of 2.53 and 3.25 µg/ml, respectively. Additionally, EGFR-IN-118 demonstrates antioxidant activity by inhibiting DPPH free radicals, with an IC50 of 10.04 µg/ml.

EGFR/CA-IX-IN-1 (Compound 14) is a dual inhibitor of epidermal growth factor receptor (EGFR) and carbonic anhydrase IX (CA-IX), with IC50 values of 5.92 nM and 63 nM, respectively. This compound exhibits significant cytotoxicity against breast cancer cells (MDA-MB-231, MCF-7) with IC50 values of 5.78 μM and 8.05 μM. Additionally, EGFR/CA-IX-IN-1 inhibits the catalytic activity of CA-IX, increases the BAX/Bcl-2 ratio, activates caspases, and causes cell cycle arrest at the G1 phase. It shows potential for breast cancer research.

EGFR/HER2-IN-18 is a stable dual inhibitor targeting EGFR and HER2, with IC50 values of 0.09 μM and 0.08 μM, respectively. It exhibits broad-spectrum anticancer activity and can induce apoptosis and inhibit the cell cycle in MCF-7 cells. EGFR/HER2-IN-18 is applicable for breast cancer research.