EGFR Inhibitor

EAI001 is a potent, selective mutant epidermal growth factor receptor (EGFR) allosteric inhibitor with an IC₅₀ value of 24 nM for EGFR^L858R/T790M. EAI001 can be used for research of cancer.

CZC-8004 (CZC-00008004) is a pan-kinase inhibitor. CZC-8004 has IC₅₀ values of 650 and 437 nM for EGFR WT and VEGFR2 V916M, respectively. CZC-8004 can be used in the study of cancer.

Tyrphostin AG 112 is an EGFR phosphorylation inhibitor.

Anvatabart is an anti-ERBB2 human IgG1 κ monoclonal antibody. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).

Losatuxizumab is an anti-EGFR monoclonal antibody. Losatuxizumab binds to EGFR with EC₅₀s of 0.96 nM for EGFR wild-type, 0.09 nM for EGFR^C271A,C283A, 0.12 nM for EGFRvIII, 0.66 nM for EGFR1-501. Losatuxizumab can be used for research of EGFR-expressing cancers.

AG1557 is a specific and ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, has a pIC₅₀ value of 8.194.

EGFR-IN-24 is a selective EGFR triple mutant inhibitor with >300 nM IC₅₀ against human EGFR^{del19/T790M/C797S}, EGFR^{L858R/T790M/C797S}, and EGFR^WT. EGFR-IN-24 can be used for the research of non-small cell lung cancer.

(E/Z)-AG490 ((E/Z)-Tyrphostin AG490) is a racemic compound of (E)-AG490 and (Z)-AG490 isomers. (E)-AG490 (HY-12000) is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.

Fidasimtamab is a bispecific antibody targeting human epidermal growth factor receptor 2 (Her2) and programmed death protein 1 (PD-1), with a K_a of 3.55e-10 M for human Her2 and a K_a of 1.17e-9 M for human PD-1. Fidasimtamab cross-links Her2-positive tumor cells with PD-1-positive T cells to form immune synapses, blocks PD-1-ligand interactions, preserves antibody-dependent cellular cytotoxicity, induces gasdermin B (GSDMB)-mediated pyroptosis, and activates T cells. Fidasimtamab is applicable to relevant research on Her2-positive gastric cancer.

YK-029A is an orally active inhibitor of mutant EGFR，targeting to both the T790M mutations (EGFR^T790M) and exon 20 insertion of EGFR (EGFRex20ins). YK-029A exhibits significant antitumor activity，and results tumor regression in EGFRex20ins-driven PDX models.

Afatinib (Standard) is the analytical standard of Afatinib. This product is intended for research and analytical applications. Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.

Tyrphostin AG30 (AG30) is a potent and selective EGFR tyrosine kinase inhibitor. Tyrphostin AG30 (AG30) selectively inhibits self renewal induction by c-ErbB, and is able to inhibit activation of STAT5 by c-ErbB in primary erythroblasts.

EGFR/AURKB-IN-1 (compound 7) is a dual-targeted EGFR/AURKB inhibitor, and inhibits the phpsphorylations of ^L858R EGFR and AURKB with IC₅₀s of 0.07 and 1.1, respectively. EGFR/AURKB-IN-1 occupies the hydrophobic region I or the αC-helix out pocket of EGFR and the back pocket of AURKB, inhibiting the growth, division and metastasis of tumor cells, thus can be used for cancer research.

Istiratumab (M-6495) is bispecific monoclonal antibody targeting IGF-1R and ErbB3. Istiratumab induces IGF-1R and ErbB3 receptor degradation through the proteasome pathway Istiratumab can be used for research of cancers.

4,7-Dihydroxycoumarin is an EGFR inhibitor, estrogen receptor inhibitor, and progesterone receptor inhibitor. 4,7-Dihydroxycoumarin against breast cancer cells with an IC₅₀ velue of 18.36 μg/mL. 4,7-Dihydroxycoumarin can be used for the research of breast cancer.

Neratinib (Standard) is the analytical standard of Neratinib. This product is intended for research and analytical applications. Neratinib (HKI-272) is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC₅₀s of 59 nM and 92 nM, respectively.

JND3229 is a reversible EGFR^C797S inhibitor with IC₅₀ values of 5.8, 6.8 and 30.5 nM for EGFR^{L858R/T790M/C797S}, EGFR^WT and EGFR^L858R/T790M, respectively. JND3229 has good anti-proliferative activity and can effectively inhibit tumour growth in vivo. JND3229 can be used in cancer research, especially in non-small cell carcinoma.

EGFR-IN-87 (Compound Example 2) hydrochloride is a EGFR tyrosine kinase inhibitor. EGFR-IN-87 hydrochloride has IC₅₀ value of 3.1 nM, 1.3 nM and 7.1 nM for EGFR_d746-750, EGFR_L858R/T790 and EGFR_WT in A431 cells, respectively. EGFR-IN-87 hydrochloride can be used for cancer diseases research.

MEDI4276 Antibody is an HER2-targeted antibody, which can be used for the synthesis of the ADC molecule MEDI4276. MEDI4276 Antibody can be used in the study of cancer.

Lapatinib-d₄ is the deuterium labeled Lapatinib (HY-50898). Lapatinib 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.