her 2

pan-HER-IN-2 (Compound C6) is an orally active, reversible, broad-spectrum HER inhibitor that acts on EGFR (IC50: 0.72 nM), HER4 (IC50: 2.0 nM), EGFRT790M (IC50: 8.2 nM), and L858R (IC50: 75.1 nM). pan-HER-IN-2 induces apoptosis and has anti-tumour effects.

EGFR/HER2/DHFR-IN-2 (Compound 4b) serves as an inhibitor for EGFR, HER2, and DHFR, with IC50 values of 0.248, 0.156, and 0.138 μM, respectively. It 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. Additionally, EGFR/HER2/DHFR-IN-2 has been shown to reduce the growth of breast cancer tumors [1].

HER2/neu (654-662) GP2 acetate is derived from the human epidermal growth factor receptor 2 (HER2-Neu, 654–662). HER2/neu (654-662) GP2 acetate induces HLA-A2-restricted cytotoxic T lymphocytes reactive to various epithelial cancers.

EGFR/HER2/DHFR-IN-3 (compound 4c) serves as an efficacious dual inhibitor specifically targeting EGFR/HER2, exhibiting IC50 values of 0.138 μM for EGFR and 0.092 μM for HER2, respectively. Moreover, it demonstrates inhibition of DHFR with an IC50 of 0.193 μM. Notably, this compound induces cell cycle arrest in the S phase and triggers apoptosis in MCF7 breast cancer cells [1].

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

HER2-IN-5 is an effective inhibitor of orally active HER-2.

HER2-IN-9 is an orally active HER2 inhibitor (IC50: 0.03 μM). HER2-IN-9 inhibits the proliferation and migration of HER-2-positive breast cancer cells and can be used in breast cancer research.

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.

HER2-IN-13 (Compound 33) serves as an effective HER2 inhibitor, exhibiting an IC50 value of 8 nM, and additionally demonstrates inhibition of wt-EGFR with an IC50 of 0.40 μM [1].

HER2-IN-7 is a potent inhibitor of HER2. HER2-IN-7 has shown potential for the study of diseases associated with ErbBs, particularly HER2, including cancer.

HER2-IN-10 is a psoralen derivative that induces apoptosis. HER2-IN-10 shows anti-breast cancer activity and light-activated cytotoxicity [1].

HER2-IN-6 is a potent inhibitor of HER2. HER2-IN-6 has the potential to be investigated in wild and/or mutant EGFR and/or HER2 kinase-mediated tumors.

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-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-IN-8 (compound 34) is an inhibitor of EGFR/HER2 and DHFR with IC50 values of 0.45, 0.244 and 5.669 μM for EGFR, HER2 and DHFR, respectively. EGFR/HER2-IN-8 can be used in the cancer research that exhibits anticancer activity against several cancer cell lines with high safety profile and selectivity indices [1].

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.

HER2-IN-11 is a psoralen derivative that induces apoptosis. HER2-IN-11 shows light-activated cytotoxicity and also exhibits anti-breast cancer activity [1].

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). EGFR/HER2/CDK9-IN-3 showed significant anti-tumor effects.

EGFR/HER2-IN-7 is a highly selective and potent anticancer compound specifically designed to target MCF-7 breast cancer cells. It functions as a dual inhibitor, targeting both EGFR/HER2 kinases and DHFR (dihydrofolate reductase). Its inhibitory activities are measured with IC50 values of 0.18 μM for EGFR, 0.146 μM for HER2, and 0.907 μM for DHFR [1].

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

EGFR/HER2-IN-2 (Compound ZINC35560729) is a dual EGFR and HER2 inhibitor that acts on both EGFR (IC50: 5.02 μM) and HER2 (IC50: 0.83 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/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/DHFR-IN-1 is a highly selective and potent anticancer compound specifically targeting MCF-7 breast cancer cells. It acts as a multi-inhibitor, targeting the EGFR/HER2 kinase and DHFR enzymes, with IC50 values of 0.153 μM, 0.108 μM, and 0.291 μM, respectively. Its mechanism of action involves cell cycle arrest at the G1/S phase and induction of apoptosis in cells [1].

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.

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.

HER2-IN-14 (Compound 34) is a potent inhibitor of HER2, achieving an inhibitory concentration (IC50) of 18 nM. Additionally, this compound exhibits inhibitory activity against wild-type EGFR (wt-EGFR) with an IC50 of 6.3 μM [1].

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

PF-04929113 Mesylate (SNX-5422 Mesylate), a prodrug of SNX-2112, is an orally available Hsp90 inhibitor (Kd: 41 nM) and also induces Her-2 degradation (IC50: 37 nM).

(-)-Epigallocatechin Gallate (EGCG) is an antioxidant polyphenol flavonoid that inhibits telomerase and DNA methyltransferase. (-)-Epigallocatechin Gallate (EGCG) blocks the activation of EGF receptors and HER-2 receptors. (-)-Epigallocatechin Gallate (EGCG) is a phenolic antioxidant found in a number of plants such as green and black tea. It inhibits cellular oxidation and prevents free radical damage to cells.

Affibody (affibody) ligands that are specific for the extracellular domain of human epidermal growth factor receptor 2 (HER2/neu) have been selected by phage display technology from a combinatorial protein library based on the 58 amino acid residue staphy

XMT-1519 conjugate-1 (compound 31) serves as a linker for the HER-2 monoclonal antibody XMT-1519, facilitating the synthesis of antibody-drug conjugates (ADCs) to enhance antitumor activity [1].

Coenzyme Q0 (CoQ0), a potent, orally active ubiquinone compound derived from Antrodia cinnamomea, induces apoptosis and autophagy. It suppresses HER-2/AKT/mTOR signaling, enhancing apoptosis and autophagy mechanisms. Additionally, Coenzyme Q0 regulates NFκB/AP-1 activation and promotes Nrf2 stabilization, contributing to the attenuation of inflammation and redox imbalance. It also exhibits anti-angiogenic activity by downregulating MMP-9/NF-κB and upregulating HO-1 signaling.

PROTAC IDO1 Degrader-1, a pioneering compound, efficiently targets indoleamine 2,3-dioxygenase 1 (IDO1) for ubiquitination and degradation by recruiting IDO1 to the CRBN E3 ligase, thereby facilitating its entry into the ubiquitin-proteasome system (UPS) with a DC50 of 2.84 μM. This compound also moderately enhances the tumor-killing efficacy of HER2 CAR-T cells[1].

ERα degrader-2 is a selective and potent estrogen receptor (SERD) degrader with anticancer activity, inhibits ERα, and has an EC50 value for estrogen receptor degradation of 0.3 nM.ERα degrader-2 can be used for the prevention and treatment of HER-positive breast cancer.

Neratinib dimethylamine N-oxide is an irreversible inhibitor of the HER-2 receptor tyrosine kinase with potential antineoplastic activity.

Neratinib pyridine N-oxide is an irreversible inhibitor of the HER-2 receptor tyrosine kinase with potential antineoplastic activity.

EGFR-IN-16 (AG473) is an inhibitor of EGFR in human A431 cells.

SU-4312, also known as DMBI, is a potent and selective inhibitor of VEGFR and PDGFR tyrosine kinases (IC50 values are 0.8 and 19.4 μM respectively). SU4312 (SU 4312) unexpectedly protects against MPP(+) -induced neurotoxicity via selective and direct inhibition of neuronal NOS.

Disitamab vedotin (RC-48) is an antibo-active molecular conjugate (ADC) containing a monoclonal antibody against human epidermal growth factor receptor 2 (HER2) that binds to the cytotoxic agent MMAE via a degradable linker. Disitamab vedotin showed anti-tumor and anti-proliferation activities in gastric cancer cells with different HER-2 expression levels, and inhibited the expression of HER-2 protein in gastric cancer cells.

BMS-690514 is a potent and orally active inhibitor of EGFR and VEGFR. It has IC50s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively.

Neratinib maleate monohydrate is an irreversible inhibitor of the HER-2 receptor tyrosine kinase with potential antineoplastic activity.

EGCG Octaacetate, a prodrug of EGCG, is utilized to enhance the stability and bioavailability of EGCG in vivo. It has high efficacy, bioavailability, anti-oxidation, and anti-angiogenesis capacities.