EGFR Inhibitor

Olafertinib (CK-101) is an orally available, third generation and irreversible epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI). Olafertinib selectively inhibits both EGFR-TKI-sensitizing and resistance mutations with minimal activity on wild-type EGFR. Olafertinib can be used in research for non-small cell lung cancer (NSCLC) with EGFR mutations and other advanced malignancies.

JCN037 (JGK037) is non-covalent and BBB-penetrant EGFR tyrosine kinase inhibitor, with IC₅₀ values of 2.49 nM, 3.95 nM, 4.48 nM for EGFR, p-wtEGFR and pEGFRvⅢ, respectively.

PKI-166 is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC₅₀ of 0.7 nM.

EGFR-IN-86 (compound 4i) is an EGFR inhibitor (IC₅₀: 1.5 nM) with high activity against glioblastoma. EGFR-IN-86 induces apoptosis and arrests the U87 cell cycle in the G2/M phase.

EGFR ligand-9 is an EGFR ligand. EGFR ligand-9 can be used for synthesis of PROTAC EGFR degrader 9 (HY-161536).

Tyrphostin A51 is a potent protein tyrosine kinase (PTK) inhibitor. Tyrphostin A51 inhibits the volume-dependent release of [³H]taurine in a dose-dependent manner. Tyrphostin A51 markedly reduces cellular tyrosyl phosphorylation level. Tyrphostin A51 inhibits both basal and EGF-induced human bone cell proliferation.

WZ8040 is an irreversible mutated EGFR T790M inhibitor and inhibits EGFR phosphorylation. WZ8040 displays 100-fold greater activity against the mutated EGFR than the normal.

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

Futuximab is a chimeric monoclonal antibody targeting non-overlapping epitopes on EGFR. Futuximab has antineoplastic activity.

EGFR Human Pre-designed siRNA Set A contains three designed siRNAs for EGFR gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Nezutatug (HMBD-001) is a humanized IgG1 monoclonal antibody inhibitor targeting HER3. Nezutatug inhibits the dimerization of HER3 and inhibits the growth, proliferation and other activities of tumor cells. Nezutatug is promising for research of cancers, such as pancreatic cancer and non-small cell lung cancer.

EGFR-IN-98 (Compound 4c) is a EGFR inhibitor. The IC₅₀ values of L858R/T790M/C797S and Del19/T790M/C797S are 0.277 μM and 0.089 μM, respectively. EGFR-IN 98 can be used in the study of tumors.

RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC₅₀ of 4 μM.

RTC-5 (TRC-382) is an optimized phenothiazine with anti-cancer potency. RTC-5 demonstrates efficacy against a xenograft model of an EGFR driven cancer, its effects is attributed to concomitant negative regulation of PI3K-AKT and RAS-ERK signaling.

CCT365623 hydrochloride is an orally active lysyl oxidase (LOX) inhibitor, with an IC₅₀ of 0.89 μM. CCT365623 hydrochloride suppresses EGFR (pY1068) and AKT phosphorylation driven by EGF. CCT365623 hydrochloride is extremely well tolerated, and has good pharmacokinetic properties.

(E)-AG 556 is a highly selective EGFR inhibitor and also blocks LPS-induced TNF-α production.

Epitinib (HMPL-813) is a selective, orally active, blood-brain barrier-permeable EGFR tyrosine kinase inhibitor. Epitinib is applicable to research on EGFR^T790M-positive non-small cell lung cancer with brain metastasis and advanced solid tumors.

EGFR-IN-8 is a dual EGFR and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC.

Dosimertinib mesylate is a potent and orally active EGFR inhibitor. Dosimertinib mesylate decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib mesylate shows antiproliferative and anti-tumor activity. Dosimertinib mesylate has the potential for the research of non-small-cell lung cancer (NSCLC).

Tomuzotuximab (Anti-Human EGFR Recombinant Antibody) is a fully human glycoengineered IgG1 monoclonal antibody against EGFR. Tomuzotuximab has anticancer effects.