EGFR Inhibitor

Anti-Epiregulin Antibody is an anti-Epiregulin antibody. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).

EGFR-IN-173 is an orally active, pan-mutant EGFR tyrosine kinase inhibitor that targets EGFR 19del, L858R/T790M and C797S triple-mutations, potently inhibiting EGFR^{19del/T790M/C797S} with an IC₅₀ of 1.19 nM while showing over 100-fold selectivity for mutant over wild-type EGFR (IC₅₀ = 19.362 μM against WT). EGFR-IN-173 significantly inhibits cell migration, induces apoptosis in non-small cell lung cancer (NSCLC) cells. EGFR-IN-173 inhibits EGFR phosphorylation and suppresses the downstream pathways (MAPK/ERK, AKT, STAT3). EGFR-IN-173 exhibits antitumor efficacy in NSCLC and Ba/F3 xenograft models. EGFR-IN-173 can be used for NSCLC research.

EGFR T790M/L858R-IN-9 (Compound 8) is an EGFR-L858R/T790M inhibitor that demonstrates potent inhibitory phosphorylation effects against the EGFR-L858R/T790M mutant kinase, with an IC₅₀ value of 0.0064µM. EGFR T790M/L858R-IN-9 also inhibits the proliferation of non-small cell lung cancer (NSCLC) cells and can be utilized in cancer research.

HER4/HER2-IN-1 (Compound 4b) is a HER4/HER2 inhibitor. HER4/HER2-IN-1 inhibits the proliferation of HER2-positive cells. HER4/HER2-IN-1 reduces the total expression level of HER2 in A431 cells, while the phosphorylated HER2 (p-HER2) does not decrease. HER4/HER2-IN-1 lowers the level of cell cycle protein D1 (cyclin D1) and stimulates the cleavage of PARP. HER4/HER2-IN-1 can be used for the study of cancer, such as breast cancer.

EGFR/HDAC-IN-2 (Compound 38) is dual-functional inhibitor of EGFR and HDAC3 with IC₅₀s of 20.34 and 1.09 nM for CDK9 and HDAC3, respectively. EGFR/HDAC-IN-2 has superior anti-proliferative activity against cancer cells, inhibits cell migration and induces late-stage cell apoptosis. EGFR/HDAC-IN-2 significantly inhibits triple-negative breast cancer (TNBC) tumor growth in xenograft mouse models. EGFR/HDAC-IN-2 can be used for cancers like TNBC research.

NGI‑189 is a selective OST‑A inhibitor. NGI‑189 inhibits the STT3A catalytic subunit of the OST complex and reduces N‑glycosylation of target glycoproteins. NGI‑189 blocks oncogenic and bypass signaling, reduces phosphorylation of EGFR, AKT, p70S6K and S6RP, and induces cell cycle arrest and apoptosis. NGI‑189 markedly suppresses tumor growth and induces tumor regression in non‑small cell lung cancer (NSCLC) xenograft models. NGI‑189 can be used for the research of EGFR‑mutant non‑small cell lung cancer.

EGFR-IN-136 (compound 21v) is a potent EGFR inhibitor with IC₅₀ values of 20.2, 1.2, 2.3, 12.5 nM for EGFR^WT, EGFR^LR/TM, EGFR^19D/TM/CS, EGFR^LR/TM/CS, respectively. EGFR-IN-136 shows antiproliferative activity. EGFR-IN-136 shows antitumor activity and has the potential for the research of NSCLC.

Cyasterone (Standard) is the analytical standard of Cyasterone. This product is intended for research and analytical applications. Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). Cyasterone manifests anti-proliferation effect by induced apoptosis and cell cycle arrests. Cyasterone may serves as a therapeutic anti-tumor agent against human tumors.

EGFR-IN-145 (compound 7c) is an EGFR kinase inhibitor. At a concentration of 20 μM, EGFR-IN-145 has an inhibition rate of 52.7% on EGFR-wild type kinase.

NSC81111 is a potent and orally active EGFR-TK inhibitor with an IC₅₀ of 0.15 nM. NSC81111 has anticaner effects.

Neptinib (NEP010) is an orally active derivative of Afatinib (HY-10261) that has stronger antitumor activity than Afatinib (HY-10261) by improving pharmacokinetics. Neptinib has a significant inhibitory effect on tumor growth in mouse non-small cell lung cancer models with different EGFR mutations. Neptinib has a certain inhibitory effect on the EGFR kinase family, with IC₅₀ values ??of 0.24 nM, 7.25 nM, 0.46 nM and 1.79 nM for EGFR^wt, EGFR^L858R/T790M, EGFR^L858R and EGFR^T790M, respectively.

4-TCPA is a potent VEGFR2 inhibitor. 4-TCPA induces apoptosis and cell cycle arrest, likely through inhibition of VEGFR2 and EGFR signaling with additional effects on the mTOR pathway. 4-TCPA can inhibit the vitality and proliferation of various cancer cell lines. 4-TCPA can be used for the study of cancers such as lung cancer, breast cancer and leukemia.

Paeciloquinone D can inhibit the EGFR protein tyrosine kinase.

BML-265 is a potent EGFR tyrosine kinase inhibitor. BML-265 disrupts Golgi integrity and abolishes secretory protein transport of diverse cargos. BML-265 affects Golgi integrity and transport in human cells but not in rodent cells.

Tyrphostin AG17 is an orally active CDK2 inhibitor and EGFR tyrosine kinase antagonist. Tyrphostin AG17 reduces the levels of p21 and p16. Tyrphostin AG17 induces G1 phase cell cycle arrest, Apoptosis, mitochondrial dysfunction, decreased ATP levels, and inhibits DNA, RNA and protein synthesis, adipogenesis, and lipid synthesis. Tyrphostin AG17 inhibits fat accumulation, white adipose tissue hypertrophy, and alterations of glycogen and lipid inclusions in hepatocytes in obese mice without changing their serum biochemical parameters. Tyrphostin AG17 exhibits anticancer effects. Tyrphostin AG17 can be used in research related to immunoblastic lymphoma, leukemia, ovarian cancer, glioblastoma, colon cancer, breast cancer, melanoma, obesity and hepatic steatosis.

WHI-P180 (Janex 3) is a multi-kinase inhibitor; inhibits RET, KDR and EGFR with IC₅₀s of 5 nM, 66 nM and 4 μM, respectively.

BIM-46174 is a heterotrimeric G protein complex inhibitor. BIM-46174 blocks GPCR downstream signaling by trapping Gα proteins in a nucleotide-free pocket conformation, thereby inhibiting Gαq-mediated calcium release, Gαs-mediated cAMP production, and GPCR-regulated cancer cell invasion. In vitro, BIM-46174 effectively suppresses a variety of clinically multidrug-resistant cell lines and induces tumor cell apoptosis through activation of caspase-3 and PARP cleavage. BIM-46174 also inhibits activation of the Neu1-MMP-9-GPCR signaling platform and downstream NF-κB signaling, and is widely used in the study of cancer signaling pathways and inflammation-related research, including lung cancer, pancreatic cancer, breast cancer, melanoma, and leukemia.

Tyrphostin 63 (compound 13) is an epidermal growth factor receptor (EGFR) inhibitor with IC₅₀ and K_i values are 375 and 123 μM, respectively.

Tesevatinib (Standard) is the analytical standard of Tesevatinib. This product is intended for research and analytical applications. Tesevatinib (XL-647) is an orally available, blood-brain barrier-penetrant inhibitor of the epidermal growth factor receptor (EGFR). Tesevatinib significantly reduces cellular viability, with IC50 values of 11 nM and 102 nM in GBM12 and GBM6, respectively. Tesevatinib also inhibits HER2 (IC50=16.1 nM), VEGFR2 (IC50=1.5 nM), and Src (IC50=10.3 nM). Tesevatinib can inhibit tumor proliferation and exhibits antitumor activity.

SYR127063 is a potent and selective human epidermal growth factor receptor 2 (HER2) tyrosine kinase inhibitor with an IC₅₀ of 11 nM. SYR127063 binds to the active site of the HER2 kinase domain in an ATP-competitive manner, thereby preventing the formation of the conserved salt bridge required for kinase activation. SYR127063 can be used in research related to breast cancer, ovarian cancer and gastric cancer.