EGFR

<p>EGFR-IN-74 is a potent inhibitor targeting EGFR, specifically effective against the L858R/T790M mutations, exhibiting an IC50 value of 138 nM.</p>

<p>MS 154 is a potent PROTAC® targeting mutant EGFR in lung cancer, sparing WT-EGFR; effective in mice, with DC50 of 11-25 nM.</p>

<p>EGFR-IN-33, a low-toxicity acrylamide, inhibits EGFR, aiding against cancer, especially NSCLC (from WO2021185348A1, comp. 13).</p>

<p>Nazartinib is an EGFR inhibitor. Nazartinib S-enantiomer is the less active S-enantiomer of Nazartinib.</p>

<p>EGFR-IN-1: an oral, irreversible EGFR inhibitor targeting L858R/T790M mutations with high selectivity, showing potent antitumor effects.</p>

<p>Simotinib (AL-6802) is an EGFR tyrosine kinase inhibitor (IC50 : 19.9 nM) with antitumour activity for the study of non-small cell lung cancer.</p>

<p>Sevabertinib (BAY 2927088) is an EGFR tyrosine kinase inhibitor, with anticancer activity, used in research on non-small cell lung cancer.</p>

<p>EGFR-IN-1 HCl targets L858R/T790M EGFR mutants over wild-type; IC50: 4 nM in H1975, 28 nM in mutant HCC827 cells.</p>

<p>EGFR-IN-87 is an EGFR tyrosine kinase inhibitor with potent inhibitory activity, exhibiting IC50 values of 3.1 nM, 1.3 nM, and 7.1 nM against EGFR_d746-750,</p>

<p>BGB-8035 is a BTK inhibitor with antitumor activity that inhibits BTK, TEC, and EGFR.BGB-8035 is used in the study of tumors and autoimmune diseases.</p>

<p>EGFR/ErbB-2 inhibitor-1 is a selective ErbB2/HER2 inhibitor that effectively blocks ErbB2 and HER2 signaling.</p>

<p>EGFR-IN-8, a dual inhibitor targeting both EGFR and c-Met, shows potential as a promising candidate for further development in treating EGFR TKI-resistant NSCLC</p>

<p>BML-265 is a potent inhibitor of EGFR tyrosine kinase (EGFR tyrosine kinase). It disrupts Golgi apparatus integrity in human cells and hinders the transport of secretory proteins across various substances. In contrast, BML-265 does not affect the integrity and transport of the Golgi apparatus in rodent cells.</p>

<p>EGFR-IN-35, an acrylamide-based EGFR inhibitor, shows promise for EGFR mutation-related cancers like NSCLC.</p>

<p>EGFR/HER2-IN-8 inhibits EGFR, HER2, DHFR (IC50: 0.45, 0.244, 5.669 μM); useful in cancer research, safe and selective.</p>

<p>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.</p>

<p>JBJ-09-063: EGFR inhibitor, IC50s 0.147-0.396 nM for various mutants; hinders EGFR/Akt/ERK1/2 phosphorylation; targets TKI-sensitive/resistant lung cancer.</p>

<p>HER2-IN-9, an oral HER2 inhibitor (IC50: 0.03 μM), hinders growth and spread of HER2+ breast cancer.</p>

<p>JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active inhibitor of EGFR with an IC 50 of 15 nM for EGFR L858R/T790M [1].</p>

<p>EGFR-IN-135 (compound 3d) is an EGFR inhibitor with an IC50 value of 0.086 µM. It inhibits cell growth and arrests the cell cycle in the S phase in breast cancer cell lines.</p>

<p>HER2-IN-8 is an inhibitor of HER-2 that can be used in the study of cancer and inflammation-related diseases.</p>

<p>EGFR/HER2-IN-7: Potent, selective dual inhibitor for MCF-7 cancer; IC50: EGFR 0.18μM, HER2 0.146μM, DHFR 0.907μM.</p>

<p>EGFR-IN-48: potent EGFR inhibitor, oral, IC50: 0.193-66.7 nM, blocks EGFR mutants &amp; BaF3/PC-9 cell proliferation.</p>

<p>Sacibertinib inhibits Trk, targeting EGFR-TK (EC50 110 nM) &amp; HER2 (EC50 244 nM), with anticancer properties.</p>

<p>EGFR-IN-17: potent, selective EGFR inhibitor, IC50 of 0.2 nM, overcomes C797S drug resistance.</p>

<p>EGFR-IN-38: low-toxic acrylamide-derived EGFR inhibitor, targets NSCLC, patented for research on EGFR mutation-related diseases.</p>

<p>EGFR-IN-126 (compound 9d) is an effective inhibitor of EGFR L858R/T790M/C797S, displaying an IC50 value of 0.005 μM. It exhibits antitumor activity both in vivo and in vitro.</p>

<p>EGFR-IN-149 (Compound 3-OH) is an EGFR inhibitor with an IC50 value of 0.42 nM.</p>

<p>EGFR-IN-160 is an EGFR inhibitor with IC50 values of 1.62, 0.49, and 0.98 μM for EGFRWT, EGFRT790M, and EGFRL858R/T790M/C797S, respectively. It can induce cell cycle arrest at the G2/M and S phases and apoptosis (Apoptosis) in NCI-H522 cells, demonstrating anticancer properties. Additionally, EGFR-IN-160 exhibits antioxidant activity against DPPH (IC50: 12.11 µM) and H2O2 (IC50: 8.89 µM).</p>

<p>Potent EGFR/HER2/DHFR inhibitor for MCF-7 breast cancer; IC50: 0.153/0.108/0.291 μM; arrests G1/S phase, triggers apoptosis.</p>

<p>EGFR-IN-18 strongly inhibits L858R/T790M/C797S mutant EGFR (4.9 nM) and also targets wild-type EGFR (47 nM).</p>

<p>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.</p>

<p>EGFR/BRAF-IN-1 inhibits EGFR/BRAF (BRAFV600E IC50: 45 nM, GI50: 35 nM) and has antioxidant properties.</p>

<p>Andamertinib is an EGFR inhibitor with antitumor activity.</p>

<p>EGFR-IN-125 (example 37) is a potent EGFR inhibitor with IC50 values of &lt;0.3 nM for EGFR(d746-750/T790M/C797S), 0.52 nM for EGFR(L858R/T790M/C797S), 0.5 nM for EGFR(d746-750/C797S), 0.69 nM for EGFR(L858R/C797S), and 0.92 nM for EGFR (wild type).</p>

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

<p>HER2-IN-7 is a potent HER2 inhibitor with potential for researching ErbB-related diseases, especially cancer.</p>

<p>Tarloxotinib bromide (TH-4000) is an irreversible inhibitor of EGFR/HER2.</p>

<p>Neptinib (NEP010), a derivative of Afatinib, exhibits enhanced antitumor properties and improved pharmacokinetics when administered orally. It demonstrates a notable suppression of tumor expansion in mouse models of non-small cell lung cancer harboring various EGFR mutations. Furthermore, Neptinib effectively inhibits the EGFR kinase family, exhibiting IC 50 values of 0.24 nM for EGFR wt, 7.25 nM for EGFR L858R/T790M, 0.46 nM for EGFR L858R, and 1.79 nM for EGFR T790M.</p>

<p>HER2-IN-21 (compound 657994) is an inhibitor of the human epidermal growth factor receptor 2 (HER2) with an IC50 value of 3.85 μM.</p>

<p>NSC381467: Potent, oral EGFR-TK inhibitor with strong antiproliferative effects, promising for cancer research.</p>

<p>EGFR-IN-23, identified as compound 8 in WO2021244502A1, is a potent EGFR tyrosine kinase inhibitor (TKI) demonstrating an inhibitory concentration (IC50) of 8.</p>

<p>EGFR/HER2-IN-4: oral, irreversible dual EGFR inhibitor (IC50: 0.6 nM), targets L858R/T790M mutations, potent anti-lung cancer effects in vivo.</p>

<p>EGFR/HER2-IN-5: Irreversible, oral dual EGFR inhibitor, IC50 0.6 nM, targets L858R/T790M mutations, anti-tumor in vivo for lung cancer study.</p>

<p>BPI-15086 is an orally active, effective, irreversible inhibitor selective for mutations, targeting both EGFR and the T790M resistance mutation tyrosine kinase. It can be utilized in the study of non-small cell lung cancer.</p>

<p>ES-072, a selective inhibitor targeting the EGFR mutant (EGFR-T790M), is administered orally. By hindering EGFR-T790M activity, it activates GSK3α, which subsequently leads to the phosphorylation of PD-L1 at Ser279 and Ser283. This phosphorylation facilitates the recruitment of the E3 ubiquitin ligase ARIH1, resulting in the ubiquitination and proteasomal degradation of PD-L1. Such a process not only curtails the growth of cancer cells but also amplifies the anti-tumor immune response by diminishing PD-L1 levels. ES-072 has shown efficacy in impeding the proliferation of non-small cell lung cancer (NSCLC) cells.</p>

<p>SST0116CL1 is an HSP90 inhibitor (IC50: 0.21 μM) that targets the ATP-binding pocket of Hsp90, disrupting its chaperone function and leading to the degradation of client proteins (EGFR, CDK4, and AKT). It induces the degradation of Her2 in BT-474 cells (IC50: 0.2 μM) and exhibits antiproliferative activity, inhibiting tumor growth.</p>

<p>EGFR-IN-139 (compound PD 18) is an EGFR inhibitor with IC50 values of 12.88 nM (wild type), 10.84 nM (L858R/T790M), and 42.68 nM (L858R/T790M/C797S). It demonstrates significant anticancer activity against the A549 and H1975 cancer cell lines, which express high levels of EGFR. EGFR-IN-139 exhibits strong selectivity for cancer cells and can be utilized in research on non-small cell lung cancer (NSCLC).</p>

<p>HER2-IN-6, a potent HER2 inhibitor, may target wild/mutant EGFR and HER2-mediated tumors. (Patent WO2021164697A1, compound 11)</p>

<p>HER2-IN-12 is an HER2 inhibitor with an IC50 value of 121 nM and can be used to study cancers such as breast cancer.</p>