egfrin5

EGFR-IN-5 is a selective inhibitor of EGFR. The IC50s for EGFR, EGFR(L858R), EGFR(L858R/T790M), and EGFR(L858R/T790M/C797S) are 10.4, 1.1, 34, 7.2 nM, respectively.

EGFR-IN-542 is a novel EGFR inhibitor. EGFR-IN-542 significantly reduces myocardial inflammation, fibrosis, apoptosis and dysfunction. It shows promise for use in the treatment of obesity-induced cardiac complications.

EGFR-IN-53 (Compound 7) is a potent EGFR inhibitor (IC50 = 8.264 μM) with cytotoxic activity against cancer cell lines [1].

EGFR-IN-51 (Compound 6) is a highly potent EGFR inhibitor with IC50 values of 0.493, 102.60, and 461.63 μM against EGFR, EGFR L858R-TK, and EGFR T790M-TK targets, respectively. Additionally, EGFR-IN-51 exhibits cytotoxicity against cancer cell lines, effectively inducing apoptosis [1].

EGFR-IN-52 (Compound 4) is a highly effective inhibitor of the epidermal growth factor receptor (EGFR) with IC50 values of 0.358, 86.02, and 432.67 μM against EGFR, EGFR L858R-TK, and EGFR T790M-TK, respectively. Additionally, it demonstrates potent cytotoxic effects on cancer cell lines and triggers apoptosis [1].

EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR tyrosine kinase (EGFR-TK) inhibitor with an IC50 of 0.054 μM. It also inhibits VEGFR-2, CK2α, topoisomerase IIβ, and tubulin polymerization with IC50 values of 0.087, 0.171, 0.13, and 3.61 μM, respectively. The compound promotes cell cycle arrest at the G2/M and pre-G1 phases and induces apoptosis in cancer cells [1].

EGFR-IN-54 (Compound 3c) is a potent EGFR inhibitor (IC50: 1.623 μM) with cytotoxicity against cancer cells.

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.

EGFR-IN-59 is a potent and selective EGFR inhibitor. It downregulates PI3K/AKT/mTOR signaling by blocking receptor autophosphorylation, exhibiting significant anti-proliferative activity in A431 and NSCLC cells.

EGFR-IN-55 is a potent inhibitor of EGFR, acting on EGFRWT (IC50: 70 nM) and EGFRL858R/T790M (IC50: 3.9 nM). EGFR-IN-55 was able to block the cell cycle of NCI-H1975 cells in G0/G1 phase, exhibiting anticancer effects.

EGFR-IN-58 is a potent, selective, ATP-competitive inhibitor of EGFR. EGFR-IN-58 exhibits significant cytotoxicity against melanoma, colon and blood cancers.

EGFR-IN-50 is a potent EGFR inhibitor targeting L858R resistance mutations, acting on TEL-EGFR-L858R-BaF3 and TEL-EGFR-T790M-L858R-BaF3 with GI50 values of 8 nM and 6.03 μM, respectively. EGFR-IN-50 exhibits anti-proliferative effects on cancer cells. .

Diethanolamine Fusidate is a bacteriostatic antibiotic with similar activity and better absorption after oral administration (in animals) than the sodium salt of Fusidic Acid. This product inhibits protein synthesis in prokaryotes by inhibiting the ribosome-dependent activity of G factor and translocation of peptidyl-tRNA.

EGFR-IN-557 is an EGFR inhibitor, attenuating Ang II-induced Kidney Fibrosis.

VEGFR-IN-5 (compound 9k) is an effective inhibitor of VEGFR2 with an IC50 of 8.4 nM, exhibiting moderate oral bioavailability. It inhibits migration and invasion of human umbilical vein endothelial cells (HUVEC) and induces apoptosis.