egfr-in-5

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 VEGFR2-IN-5 (Compound 14) is an orally active dual inhibitor of EGFR and VEGFR2, exhibiting an IC50 value of 1.15 µM for VEGFR2 and 0.28 µM for EGFRT790M. This compound demonstrates significant anticancer activity.

EGFR-TK-IN-5 (Compound NCE 2) is a thiazolyl pyrazoline derivative with significant inhibitory activity and stability against EGFR. It is applicable in tumor research.

EGFR/BRAFV600E-IN-5 (Compound 7I) is a dual inhibitor targeting both BRAFV600E and EGFR, with IC50 values of 0.048 μM and 0.037 μM, respectively. It exhibits potent anti-melanoma activity, showing IC50 values of 3.16 μM for MALME-3M cells and 2.50 μM for LOX-IMVI cells. The compound exerts its antitumor effects by inducing G1 phase arrest, inhibiting DNA synthesis, and activating the mitochondrial apoptosis pathway. EGFR/BRAFV600E-IN-5 is useful for melanoma research, especially in studies focusing on the combined inhibition of the BRAFV600E mutation and EGFR signaling pathways.

EGFR/HER2-IN-5 is an irreversible, orally active dual inhibitor of EGFR activity (IC50: 0.6 nM). EGFR/HER2-IN-4 shows potent EGFR kinase inhibitory activity against L858R and T790M mutations. EGFR/HER2-IN-4 exhibits significant anti-tumour effects in vivo and can be used to study lung cancer.

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-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 an EGFR inhibitor with an IC50 value of 190 nM and an all-time apoptosis inducer. EGFR-IN-59 exhibited cytotoxicity against a non-small lung cancer cell line (A549) and normal lung fibroblasts (WI38) with IC50s of 8.62 and 52.6 μM, respectively. EGFR-IN-59 EGFR-IN-59 can be used to study a variety of cancers including non-small cell lung cancer (NSCLC), head and neck cancer, breast cancer and colorectal cancer.

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. .

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.

MS 39 is a highly effective, highly affinity and selective depressant of mutant epidermal growth factor receptor (EGFR) with high efficiency, high affinity and selectivity. MS 39, conjured by gefitinib to VHL ligand via a linker, effectively induced the degradation of mutant EGFR (DC50 values in HCC827(exon 19 del) and H3255 (L858R mutation) lung cancer cell lines were 5 nM and 3.3 nM, respectively). However, there was no significant effect in wild-type EGFR cell lines with concentrations up to 10 μM. MS 39 inhibited the proliferation of H3255 lung cancer cells in vitro and was bioavailable in mice after administration.

EGFR mutant- in-1, A 5-methylpyrimidopyridone derivative are effective selective EGFRL858R/T790M/C797S mutant inhibitors with IC50 of 27.5 nM, which significantly weakened EGFRWT effect.

EG31 is an EGFR inhibitor that effectively suppresses the proliferation of triple-negative breast cancer (TNBC) cells by inhibiting the EGFR signaling pathway. It demonstrates a GI50 value of 498.90 nM for MDA-MB-231 cells and 740.73 nM for Hs578T cells, while also inducing apoptosis. Additionally, EG31 retains its antiproliferative activity against 5-fluorouracil (5-FU) resistant TNBC cells, with a GI50 of 519.5 nM. EG31 is applicable in research on TNBC resistance.

EGFR-IN-157 (compound IIB-5) is a potent EGFR inhibitor with an IC50 of 18.81 nM and is applicable for research in non-small cell lung cancer (NSCLC).

Icotinib Hydrochloride (BPI-2009H) is the hydrochloride salt form of icotinib, an orally available quinazoline-based inhibitor of EGFR, with potential antineoplastic activity. Icotinib selectively inhibits the wild-type and several mutated forms of EGFR tyrosine kinase. This may lead to an inhibition of EGFR-mediated signal transduction and may inhibit cancer cell proliferation. EGFR, a receptor tyrosine kinase, has been upregulated in a variety of cancer cell types.