EGFR Inhibitor

EGFR-IN-193 is an EGFR inhibitor, which can be used to synthesize PROTACs as target protein ligands, such as PROTAC EGFR degrader 17 (HY-180917).

Anticancer agent 69 (Compound 34), a potent and selective anticancer agent , potently and selectively inhibits human prostate cancer cell line PC3 (IC₅₀=26 nM). Anticancer agent 69 increases ROS level, down-regulates EGFR and induces apoptosis.

Lapatinib-d₅ is deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC₅₀ values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.

Lapatinib-d₄ (GW572016-d₄) tosylate is deuterium labeled Lapatinib (tosylate). Lapatinib (GW572016) tosylate is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC₅₀ values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.

HG-5-88-01 is an EGFR inhibitor. HG-5-88-01 exhibits no significant correlation in its anti-cancer sensitivity with the expression level of EGFR.

DS08701581 is an inhibitor of FER tyrosine kinase with IC₅₀. DS08701581 has anti-tumor activity and oral activity.

Lw13 is a Hsp90 PROTAC degrader. Lw13 induces Hsp90 degradation via the ubiquitin-proteasome system, destabilizes client proteins HER2 and AKT, and blocks the activation of the HER2/AKT/mTOR signaling pathway. Lw13 inhibits the metastasis of cervical cancer cells, induces cell cycle arrest and apoptosis (apoptosis). Lw13 exerts synergistic anti-tumor activity with Cisplatin (HY-17394). Lw13 is applicable to cervical cancer-related research.

Nimotuzumab (powder) is a humanized IgG1 monoclonal antibody targeting EGFR with a K_D value of 0.21 nM. Nimotuzumab (powder) is directed against the extracellular domain of the EGFR blocking the binding to its ligands. Nimotuzumab (powder), a strong antitumor agent, is cytolytic on target tumors by its capacity to cause antibody dependent cell mediated cytotoxicity (ADCC) and complement dependent cytotoxicity (CDC).

Apoptosis inducer 35 (Compound 6) is a multi-targeted inhibitor, that reduces the expressions of EGFR, AKT, ERK and P38-MAPKα. Apoptosis inducer 35 inhibits the proliferation of cancer cell A549 and Jurkat, arrests the cell cycle at S phase, and induces apoptosis.

Dacomitinib-d₁₀ is deuterium labeled Dacomitinib. Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC₅₀s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.

EGFR-IN-155 (compound 13a) is an EGFR inhibitor with IC₅₀ values of 0.14 nM and 0.18 nM against EGFR TK and EGFR L858R, respectively. EGFR-IN-155 inhibits tumor growth, causes a cell cycle arrest at S phase, and and induces cell apoptosis.

EGFR kinase inhibitor 4 (Compound 4) is a bivalent ATP-allosteric EGFR inhibitor (IC₅₀: 1.8 nM for mutant EGFR (LRTMCS)). EGFR kinase inhibitor 4 can be used for research of NSCLC.

EGFR-IN-144 (Compound 4B) exhibits inhibitory activities against EGFR (IC₅₀=0.639 µg/mL) and tubulin polymerization (IC₅₀=7.339 µg/mL). EGFR-IN-144 exhibits cytotoxicity in multiple cancer cell with GI₅₀ of nanomolare levels. EGFR-IN-144 downregulates the expressions of mTOR, TNF-α, and IL-6, arrests the cell cycle at G1/S phase, and induces apoptosis.

EGFR-IN-130 (compound 14b) is an EGFR inhibitor and apoptosis inducer. EGFR-IN-130 triggers death of HeLa cancer cells via apoptosis induction..

HER2-IN-19 (Compound 10e) is a potent inhibitor of HER2 and EGFR with IC₅₀ values of 0.87 respectively and 3.5 nM. HER2-IN-19 has potent inhibitory activity against tumor cells, IC₅₀^NCI-N87 = 1.63 nM, IC₅₀^BT474= 15.17 nM, IC₅₀^{BaF3-HER2YVMA} = 1.49 nM.

Zalutumumab (powder) is a high affinity, completely human IgG1 monoclonal antibody targeting EGFR. Zalutumumab (powder) binds to domain III of the EGF receptor and acts by blocking the binding of EGF and by sterically interfering with the active conformation of the receptor. Zalutumumab (powder) binds with IgG and its Fab fragment with EC₅₀s of 7 and 19 nM, respectively. Zalutumumab (powder) can be used for the research of cancer.

Anti-ERBB3/HER3 (SGP1) is a human monoclonal antibody (mAb) targeting ERBB3/HER3. Anti-ERBB3/HER3 (SGP1) inhibits Neuregulin stimulated growth of cultured breast cancer cells. Anti-ERBB3/HER3 (SGP1) can be used in breast cancer research.

EGFR/BRAFV600E-IN-3 is a EGFR, BRAFV600E and EGFRT790M inhibitor with IC₅₀ value of 57 nM, 68 nM and 9.70 nM. EGFR/BRAFV600E-IN-3 is an apoptotic inducer and also displays promising antioxidant activity.

Almonertinib-d₆ (HS-10296-d₆) is the deuterium labeled Almonertinib (HY-112823). Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC₅₀: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer.

LSD1/EGFR-IN-1 (compound L-1) is a potent inhibitor of LSD1, EGFR^T790M/L858R and EGFR^{L858R/T790M/C797S}, with IC₅₀s of 6.24 and 2.06 and 5.01 μM, respectively. LSD1/EGFR-IN-1 plays an important role in cancer research.