egfr/her2

EGFR HER2-IN-8 (compound 34) is an inhibitor of EGFR, HER2, and DHFR with IC50 values of 0.45 μM, 0.244 μM, and 5.669 μM, respectively. It demonstrates anticancer activity against several cancer cell lines, exhibiting a high safety profile and selectivity indices, making it useful for cancer research [1].

EGFR HER2-IN-7 is a highly selective and potent anticancer compound designed to target MCF-7 breast cancer cells by functioning as a dual inhibitor of EGFR HER2 kinases and DHFR (dihydrofolate reductase), with IC50 values of 0.18 μM for EGFR, 0.146 μM for HER2, and 0.907 μM for DHFR [1].

EGFR HER2 DHFR-IN-1 is a highly selective and potent anticancer compound targeting MCF-7 breast cancer cells, acting as a multi-inhibitor for EGFR HER2 kinase and DHFR enzymes, with IC50 values of 0.153 μM, 0.108 μM, and 0.291 μM, respectively. It induces cell cycle arrest at the G1 S phase and apoptosis in cells [1].

EGFR HER2-IN-6 (compound 43) is a dual EGFR HER2 and DHFR inhibitor with potent activity against EGFR kinase, HER2 kinase, and DHFR, characterized by IC50 values of 0.122 μM, 0.078 μM, and 0.585 μM, respectively. This compound displays notable anticancer properties in various cancer cell lines, while demonstrating a favorable safety profile and selectivity indices. Consequently, EGFR HER2-IN-6 holds promise as a valuable tool in cancer research [1].

EGFR HER2 CDK9-IN-1 (Compound 4) is a potent inhibitor of EGFR, HER2, and CDK9, with IC50 values of 90.17 nM, 131.39 nM, and 67.04 nM, respectively, and exhibits significant anti-tumor effects.

EGFR HER2-IN-2 (Compound ZINC35560729) is a dual inhibitor targeting EGFR (IC50: 5.02 μM) and HER2 (IC50: 0.83 μM).

EGFR HER2-IN-3 (Compound ZINC21942954) is a dual inhibitor of EGFR and HER2.

EGFR HER2 CDK9-IN-3 (Compound 10) is a potent inhibitor of EGFR (IC50:191.08 nM), HER2 (IC50:132.65 nM), and CDK9 (IC50:113.98 nM), demonstrating significant anti-tumor effects.

EGFR HER2 CDK9-IN-2 are potent inhibitors of EGFR HER2 CDK9, and they exhibited significant antitumor effects with IC50s of 145.35, 129.07 and 117.13 nM, respectively.

EGFR HER2 TS-IN-1 are EGFR, HER2 and TS (Thymidylate synthase) inhibitors with IC50 values of 0.203, 0.088 and 0.168 μM, respectively, and have the ability to induce apoptosis (MCF7 cell death).

EGFR HER2 TS-IN-2 is a potent inhibitor of EGFR (IC50: 0.173 μM), HER2 (IC50: 0.125 μM) and TS (IC50: 1.12 μM). EGFR HER2 TS-IN-2 exhibited cytotoxic effects on MDA-MB-231 cancer cells (IC50: 1.69 μM ).

EGFR HER2-IN-4 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 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 HER2-IN-9, a compound inhibiting both EGFR and HER2, demonstrates potency with IC50 values of 3.2 nM for EGFR, 14 nM for HER2, and 8.3 nM against the EGFR T790M mutation.

EGFR HER2 DHFR-IN-3 (compound 4c) is an efficacious dual inhibitor of EGFR HER2 with IC50 values of 0.138 μM for EGFR and 0.092 μM for HER2, respectively, and also inhibits DHFR with an IC50 of 0.193 μM. It induces cell cycle arrest in the S phase and triggers apoptosis in MCF7 breast cancer cells [1].

EGFR HER2 DHFR-IN-2 (Compound 4b) is an inhibitor of EGFR, HER2, and DHFR, with IC50 values of 0.248, 0.156, and 0.138 μM, respectively, and exhibits anticancer activity, displaying IC50 values of 9.14, 7.33, 14.18, 24.87, 20.07, and 6.16 μM in Hep G2, HeLa, HEp-2, HCT 116, PC-3, and MCF7 cancer cell lines, respectively; it also reduces the growth of breast cancer tumors [1].

EGFR HER2-IN-10 (compound 9F) serves as a potent, selective dual inhibitor for EGFR and HER2, exhibiting IC50 values of 2.3 nM for EGFR and 234 nM for HER2. Additionally, it demonstrates effective antiproliferative activity against prostate carcinoma [1].

EGFR HER2-IN-11 (compound 20), an orally active dual inhibitor targeting human epidermal growth factor receptor 2 (HER2) and epidermal growth factor receptor (EGFR), demonstrates IC50 values of 7.7 nM and 22 nM, respectively. This compound shows strong antitumor efficacy, specifically inhibiting the proliferation of BT-474 cancer cells with a GI50 of 601 nM [1].

EGFR HER2-IN-12 (compound 14b) serves as a dual inhibitor targeting EGFR and HER2, demonstrating 81% and 51% inhibition respectively at a concentration of 10 μM. This compound exhibits minimal toxicity towards A431 and MDA-MB-361 cancer cells [1].

EGFR HER2-IN-16 (compound 12K) is an effective dual-target inhibitor of EGFR (IC50=6.15 nM) and HER-2 (IC50=9.78 nM), exhibiting antitumor activity. This compound inhibits migration of SK-BR-3 cells, arrests the cell cycle in the G0 G1 phase, and induces cell apoptosis (apoptosis). Demonstrating strong antiproliferative properties in tumor cell models with minimal damage to healthy cells, EGFR HER2-IN-16 shows promise for research in breast cancer treatments.

EGFR HER2-IN-13 (Compd 38) serves as an inhibitor targeting mutant EGFR HER2s that show resistance to existing drugs. It is primarily utilized in cancer research.

Trastuzumab is a humanized monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab has been clinically used to treat HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer.

Zongertinib is a human HER2-selective tyrosine kinase inhibitor, a novel TK that is highly selective for covalent binding to the HER2 tyrosine kinase domain (TKD).Zongertinib exhibits antitumor activity with inhibitory effects on pHER2 and EGF.