EGFR Inhibitor

EGFR/VEGFR2-IN-7 (Compound 3e) is a dual-target EGFR/VEGFR2 inhibitor, with IC₅₀ values of 142 (EGFR) and 71 nM (VEGFR2). EGFR/VEGFR2-IN-7 exhibits broad-spectrum and potent anti-proliferative activity, especially being sensitive to breast cancer. EGFR/VEGFR2-IN-7 induces cell cycle arrest and apoptosis, inhibits cell migration and invasion. EGFR/VEGFR2-IN-7 can be used for research on breast cancer.

EphB4-IN-1 is a selective EphB4 tyrosine kinase inhibitor with IC₅₀ values of 0.16-0.30 μM. EphB4-IN-1 binds to the ATP binding site of EphB4 in a DFG-in conformation, forming four stable intermolecular hydrogen bonds. EphB4-IN-1 also inhibits Src, Abl1, Lck, and EGFR kinases. EphB4-IN-1 inhibits EphB4 autophosphorylation. EphB4-IN-1 can be used for the research of cancer, such as non small cell lung cancer.

EGFR-IN-59 (Compound 8c) is a EGFR inhibitor (IC₅₀=190 nM) and apoptosis inducer. EGFR-IN-59 exhibits cytotoxicity against non-small lung cancer cell lines (A549) and normal lung fibroblasts (WI38) with IC₅₀s of 8.62 and 52.6 µM, respectively. EGFR-IN-59 can be used for the research of various cancers such as non-small cell lung cancer (NSCLC), head and neck cancer, breast cancer and colorectal cancer.

EGFR-IN-25 is a potent EGFR inhibitor with IC₅₀s of 9 nM and 60 nM for BaF3 cells (EGFR DEL19/T790M/C797S) and A431 cells (WT), respectively.

EGFR/HER2-IN-18 is a stable EGFR/HER2 dual inhibitor with IC₅₀ values of 0.09 (EGFR) and 0.08 μM (HER2) respectively. EGFR/HER2-IN-18 exhibits broad-spectrum anti-cancer activity. EGFR/HER2-IN-18 induces MCF-7 cells apoptosis and inhibits the cell cycle. EGFR/HER2-IN-18 can be used for the study of breast cancer.

Rezivertinib (BPI-7711) hydrochloride is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib hydrochloride exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib hydrochloride has excellent central nervous system (CNS) penetration and has antitumor activity, such as non-small cell lung cancer (NSCLC).

Anticancer agent 276 (Compound 5) is a multi-target anticancer agent. Anticancer agent 276 has a potent anticancer activity against human tumor cells with IC₅₀s of 6.90 and 4.48 μM for HEPG2 and MCF7 cells, respectively. Anticancer agent 276 shows strong and stable interactions across multiple targets, including Topoisomerase II, VEGFR2, c-Met, EGFR and ERα.

(Z)-Tyrphostin A51 is the Z configuration of Lanoconazole A51. 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.

EGFR Ligand-Linker Conjugates 1 is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for EGFR (HY-150905) and a PROTAC linker, which recruits E3 ligases. EGFR Ligand-Linker Conjugates 1 can be used for synthesis of PROTAC EGFR degrader 3 (HY-144605).

EGFR-IN-196 is an EGFR inhibitor with an IC₅₀ of 105.96 nM. EGFR-IN-196 inhibits EGFR enzymatic activity, reduces phosphorylated PI3K levels, and suppresses downstream EGFR-AKT signaling. EGFR-IN-196 increases intracellular ROS generation, induces mitochondrial depolarisation, and induces apoptosis in cancer cells. EGFR-IN-196 can be used for the research of lung cancer.

Opadotina is a small molecule of anvatabart opadotin. Opadotina shows antineoplastic activity.

Yuanhuadin, extracted from Genkwa Flos Daphne genkwa, has antitumor activity through inhibiting Akt/mTOR and EGFR pathways, induce cell-cycle arrest and abortion.

EGFR/CDK2-IN-3 (compound 4b) is a dual inhibitor of EGFR and CDK-2 with IC₅₀s of 71.7 and 113.7 nM, respectively. EGFR/CDK2-IN-3 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-3 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC₅₀ of 3.16 μM.

CLM3, a pyrazolopyrimidine derivative, is a multiple tyrosine kinase inhibitor. CLM3 shows antiproliferative and proapoptotic activity on endothelial and cancer cells, synergistically enhanced by SN38 (HY-13704). These effects are mainly due to its inhibition of phosphorylation of VEGFR-2, EGFR and RET tyrosine kinases and their related signaling pathways.

EGFR-IN-58 (Compound 4a) is a potent, ATP-competitive, and selective EGFR inhibitor. EGFR-IN-58 shows potent cytotoxicity against melanoma, colon, and blood cancers.

EGFR-IN-190 (Compound 3o) is an inhibitor that targets both EGFR (IC₅₀ = 0.028 μM) and COX-2 (IC₅₀ = 0.208 μM). EGFR-IN-190 exhibits potent inhibitory activity against MCF-7 cells and induces apoptosis (apoptosis). EGFR-IN-190 can be used for research on breast cancer.

EGFR/BRAF-IN-1 (compound 21), a 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivative, is a potent EGFR/BRAF inhibitor with an IC₅₀ of 45 nM for BRAF^V600E. EGFR/BRAF-IN-1 inhibits cancer cell proliferation (GI₅₀=35 nM). EGFR/BRAF-IN-1 shows good antioxidant activity.

Khellin (Standard) is the analytical standard of Khellin. This product is intended for research and analytical applications. 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.

EGFR-IN-94 (compound 5a) is a EGFR inhibitor with IC₅₀ of 0.086?μM, and also has IC₅₀ of 0.107μM and 2.52 μM for VEGFR-2 and Topo II, respectively. EGFR-IN-94 induces cell apoptosis and arrests cell cycle at the S phase in HepG-2 cells .

Anticancer agent 357 is an orally active HER2 inhibitor. Anticancer agent 357 reduces the phosphorylation levels of HER2, AKT and GSK-3β, and downregulates the expression of β-catenin. Anticancer agent 357 inhibits the proliferation and migration of colon cancer cells with high HER2 expression, and suppresses tumor growth in xenograft models. Anticancer agent 357 can be used in colorectal cancer-related research.