her-4

(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.

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.

BGB-102 (JNJ-26483327) is a kinase inhibitor targeting FLT3 and YES1 and an antagonist targeting EGFR and VEGFR3, which may be useful in the study of macular degeneration and diseases associated with genetic disorders and malformations.

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.

Epertinib is a reversible and selective tyrosine kinase inhibitor of EGFR, HER2, and HER4 (IC50s: 1.48 nM, 7.15 nM, and 2.49 nM). It displays a strong antitumor activity.

Rilzabrutinib (PRN1008) is a small-molecule inhibitor and a reversible covalent inhibitor of Bruton's tyrosine kinase (BTK) (IC50 = 1.3 nM), featuring high selectivity, oral activity, and favorable cell permeability, exhibiting anti-inflammatory and immunomodulatory activities.

BMS-599626 (AC480) has been used in trials studying the treatment of Cancer, Metastases, and HER2 or EGFR Expressing Advanced Solid Malignancies.

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

BMS-599626 Hydrochloride (AC480 Hydrochloride) is an orally bioavailable inhibitor of the HER1, HER2, and HER4 tyrosine kinases (IC50 = 22, 32, and 190 nM, respectively) with potential antineoplastic activity, inhibiting the proliferation of tumor cells that overexpress these receptors.

BMS 599626 2HCl (873837-23-1(HCl)) (AC480 dihydrochloride) is a selective inhibitor of HER1 and HER2 (IC50s: 20 nM and 30 nM), ~8-fold less potent to HER4, >100-fold to Lck, VEGFR2, c-Kit, MET, etc.

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.

Varlitinib (ASLAN001) is a potent, reversible, small molecule pan-EGFR inhibitor with IC50 values of 7 nM for HER1, 2 nM for HER2, and 4 nM for HER4.

Anti-Her4 Antibody is an antibody targeting Her4 and can be used for life science research.

BMS-599626 2HCL (AC480 2HCl) is a BMS-599626 derivative. BMS-599626 is an orally available and selective dual inhibitor of HER1 and HER2 with IC50s of 20 and 30 nM, respectively. BMS-599626 inhibits tumor cell proliferation and has the potential to increase tumor BMS-599626 inhibits tumor cell proliferation and has the potential to increase tumor response to radiotherapy.

EGFR-IN-12 (EGFR Inhibitor) is a cell permeable and selective inhibitor of EGFR kinase (IC50: 21 nM) and blocks receptor autophosphorylation in cells.

pan-HER-IN-1 (Compound C5) is an irreversible, orally active Pan-HER inhibitor that exhibits IC50 values of 0.38 nM for EGFR, 1.6 nM for HER4, 2.2 nM for EGFR T790M/L858R, and 3.5 nM for HER2, respectively. pan-HER-IN-1 induces apoptosis and demonstrates antitumor activities.

pan-HER-IN-2 (Compound C6) is an orally active, reversible, broad-spectrum HER inhibitor that targets 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 possesses anti-tumor effects.

Larotinib mesylate hydrate is a potent, broad-spectrum, and orally active tyrosine kinase inhibitor (TKI), primarily targeting EGFR with an IC50 value of 0.6 nM.

Larotinib is an orally active, potent, and broad-spectrum tyrosine kinase inhibitor (TKI) with an IC50 of 0.6 nM for EGFR.

TAS0728 is a HER2 inhibitor, with antitumor activity

TAS-121 is an orally active, selective, covalent third-generation mutant EGFR tyrosine kinase inhibitor (EGFR-TKI). It effectively inhibits the L858R mutation (IC50=1.7 nM), Ex19del mutation (IC50=2.7 nM), L858R/T790M mutation (IC50=0.56 nM), and Ex19del/T790M mutation (IC50=1.1 nM), as well as wild-type EGFR (IC50=8.2 nM). TAS-121 also inhibits HER2 and HER4 with an IC50 of 110 nM and 2.6 nM, respectively. This compound prevents cellular proliferation by inhibiting the phosphorylation of EGFR and its downstream signaling targets, thereby inducing apoptosis. Additionally, TAS-121 demonstrates antitumor activity in xenograft models such as SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M).

(+)-Pinoresinol monomethyl ether 4-O-β-D-glucoside is a natural product.