EGFR Inhibitor

Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway. Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the EGFR/PI3K/Akt/mTOR signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases γ-H2AX levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer.

EGFR-IN-70 (compound 18j) is a potent EGFR inhibitor with IC₅₀ values of 23.6 and 307.5 nM for EGFR^LR/TM/CS and EGFR^WT, respectively. EGFR-IN-70 has anti-proliferative activity and suppresses phosphorylation of the EGFR. EGFR-IN-70 can be used for cancer research.

AZ7550 is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC₅₀ of 1.6 μM.

Anti-Human/Rat HER2 (neu) Antibody (7.16.4) is an anti-human and anti-rat HER2 IgG2a monoclonal antibody. Anti-Human/Rat HER2 (neu) Antibody (7.16.4) reduces tumor cell proliferation by inhibiting the HER2 signaling pathway. Anti-Human/Rat HER2 (neu) Antibody (7.16.4) can activate CD8⁺ T cells. Anti-Human/Rat HER2 (neu) Antibody (7.16.4) can be used for research on cancer such as breast cancer.

Rocbrutinib is an orally available, highly selective Bruton's tyrosine kinase (BTK) inhibitor, with an IC₅₀ of 0.11 nM against wild-type BTK and an IC₅₀ of 1.0 nM against C481S-mutated BTK. Rocbrutinib reduces the viability of leukemia cells, induces cytotoxicity and inhibits cell migration. Rocbrutinib can be used in research related to chronic lymphocytic leukemia, non-Hodgkin's lymphoma and mantle cell lymphoma.

Gefitinib (Standard) is the analytical standard of Gefitinib. This product is intended for research and analytical applications. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC₅₀ of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC₅₀ of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .

Beta-hydroxyisovalerylshikonin is a natural product isolated from Lithospermum erythrorhizon, acts as a potent inhibitor of protein tyrosine kinases (PTK), with IC₅₀s of 0.7μM and 1μM for EGFR and v-Src receptor, respectively. Beta-hydroxyisovalerylshikonin is effective against a wide variety of tumor cell lines, and most efficiently induces cell-death in NCI-H522 and DMS114 cells.

Osimertinib-d₆ is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC₅₀ of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.

Mavelertinib is a selective, orally available and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC₅₀s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC).

Ruserontinib (SKLB1028) is an orally active multikinase inhibitor of EGFR, FLT3 and Abl, with an IC₅₀ value of 55 nM for human FLT3, and has antitumor activity.

Anti-Human/Mouse Amphiregulin Antibody (AR37) is an antibody targeting amphiregulin (AREG), with a K_d value of 3.24 nM for the human protein and 6.40 nM for the mouse protein. Anti-Human/Mouse Amphiregulin Antibody (AR37) blocks the autocrine activation of the AREG-EGFR-ERK axis. Anti-Human/Mouse Amphiregulin Antibody (AR37) inhibits the proliferation and migration of ovarian cancer cells. Anti-Human/Mouse Amphiregulin Antibody (AR37) prolongs the survival of immunocompetent mice bearing syngeneic ovarian cancer tumors. Anti-Human/Mouse Amphiregulin Antibody (AR37) is applicable to ovarian cancer-related research.

4(3H) -quinazolinone is a fused nitrogen heterocyclic compound whose derivatives have a wide range of antimicrobial and antitumor activities.

EGFR-IN-95 (compound 5j) is an 2,4-diaminonicotinamide derivative. EGFR-IN-95 has potent inhibitory activity against EGFR del19/T790M/C797S and L858R/T790M/C797S.

Khellin is a furochromone that can be isolated from Ammi visnuga L.. Khellin is an EGFR inhibitor with an IC₅₀ of 0.15 µM. Khelline has anti-proliferative activity in vitro. Khellin has antispasmodic and coronary vasodilator effects.

Amivantamab (FUT8-KO) is an anti-EGFR-MET monoclonal antibody expressed by CHO cells with the fucosyltransferase 8 gene (FUT8) knocked out. Fucose deficiency enhances the ADCC effect of the antibody. Amivantamab (FUT8-KO) inhibits ligand binding, promotes endocytosis and degradation of receptor-antibody complexes, and induces Fc-dependent cytokinesis in macrophages and antibody-dependent cytotoxicity in natural killer cells.

BI-4732 is an orally active, reversible, ATP-competitive EGFR inhibitor with blood-brain barrier penetration. BI-4732 inhibits the kinase activity of EGFR L858R, T790M and C797S with IC₅₀ values of 1 nM while sparing EGFR wild-type. BI-4732 inhibits EGFR and reduces the phosphorylation of AKT, ERK, and S6K. BI-4732 demonstrates excellent intracranial anti-tumor efficacy in YU-1097 xenograft model harboring EGFR_E19del/T790M/C797S. BI-4732 can be used for the study of non-small cell lung cancer (NSCLC).

Dacomitinib (PF-00299804) hydrate is an orally active, irreversible pan-ErbB inhibitor. Dacomitinib hydrate can be used in the research of cancers such as metastatic non-small cell lung cancer (NSCLC).

BMS-599626 Hydrochloride (AC480 Hydrochloride) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC₅₀s of 20 and 30 nM, respectively. BMS-599626 Hydrochloride displays ~8-fold less potent to HER4 (IC₅₀=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 Hydrochloride inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy.

Modotuximab (DS 1024) is an IgG1κ-type chimeric antibody targeting human EGFR protein. Modotuximab binds non-overlapping epitopes on domain III of EGFR, a domain that is intact in EGFRvIII. Modotuximab has antitumor activity in vivo.

Enozertinib (ORIC-114) hemihydrate is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib hemihydrate exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib hemihydrate induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib hemihydrate can be used for the research of solid tumors and NSCLC.