HER

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.

Tucatinib (ONT-380) is a potent and selective HER2 inhibitor (IC50: 8 nM).

Rilzabrutinib (PRN1008) is a reversible covalent, selective, and orally active inhibitor of Bruton's Tyrosine Kinase (BTK) with an IC50 of 1.3 nM.

Pyrotinib dimaleate is a selective EGFR HER2 dual inhibitor with IC50 values ​​of 13 and 38 nM, respectively, for the treatment of HER2-positive breast cancer.

Patritumab (U3-1287) is an anti-HER3 monoclonal antibody with potential antitumor activity and inhibits phosphorylation of EGFR, HER2, HER3, ERK, and AKT.Patritumab promotes apoptosis and inhibits proliferation in non-small cell lung cancer.

CUDC-101 is a potent inhibitor of HDAC, EGFR, and HER2 with IC50s of 4.4 nM, 2.4 nM, and 15.7 nM, respectively.

Neratinib (HKI-272) (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor for HER2 and EGFR (IC50: 59/92 nM), respectively.

Epertinib hydrochloride (S-22611 hydrochloride) shows potent antitumor activity. Epertinib hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively.

Zenocutuzumab (MCLA-128) is a humanized antibody targeting the extracellular domains of HER2 and HER3. It can be used for research on tumors driven by NRG1 gene rearrangement.

BI-4142 is an orally active, potent and selective HER2 inhibitor that inhibits cancer cell proliferation, suppresses her2-dependent cell lines and inhibits downstream signalling.

MC-Val-Cit-PAB-Amide-TLR7 agonist 4 Conjugate is a conjugate of MC-Val-Cit-PAB-Amide and TLR7 agonist 4, used in cancer research.

Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.

Mollugin (Rubimaillin) may be a JAK2 inhibitor and inhibits LPS-induced inflammatory responses by blocking the activation of the JAK-STAT pathway. Mollugin as a candidate for a chemotherapeutic agent in OSCCs via the upregulation of the HO-1 and Nrf2 pathways and the downregulation of NF- κ B. Mollugin may be a novel therapeutic candidate for bone loss-associated disorders including osteoporosis, rheumatoid arthritis, and periodontitis. Also, it has anticancer efficacy, can modulate the HER2 pathway in HER2-overexpressing Y cells with a potential role in the treatment and prevention of human breast and ovarian Y with HER2 overexpression.

SYR127063 (BDBM-92454) (BDBM92454) is a potent and selective HER2 inhibitor, binds to HER2 in a reactive conformation.

ARRY-380 analog (HER2-Inhibitor-1) is a potent and selective HER2 inhibitor.

(S)-Afatinib (BIBW2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 0.4 10 14 1 nM for EGFRwt, EGFR (L858R), EGFR (L858R T790M), HER2, and HER4, respectively.

Poziotinib (NOV120101)(NOV120101; HM781-36B) is an irreversible HER1 2 4 inhibitor (IC50s: 3 5 23 nM).

BMS-690514 is a potent, orally active inhibitor of EGFR and VEGFR, with IC50 values of 5 nM for EGFR, 20 nM for HER 2, and 60 nM for HER 4.

1. Furanodienone has effects on MCF-7 cells are mediated, at least in part, by inhibiting ERα signaling. 2. Furanodienone inhibits EGFR/HER2 signaling pathway in BT474 and SKBR3 cells, the effect is specifically dependent on the expression of HER2 but not EGFR .

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).

Tarloxotinib bromide (TH-4000) is an irreversible inhibitor of EGFR HER2.

Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active, and selective HER2 inhibitor with an IC50 of 8 nM.

TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1 2 than HER4, less potent to MEK1 5, c-Met, Aurora B, Lck, CSK etc. Phase 1.

(S)-Sunvozertinib (DZD9008) is a rationally designed selective, irreversible EGFR/HER2 inhibitor.