EGFR/HER2

Cat. No.

A24033

CAS No.

2660250-10-0

BLU-945 (ZL-2313)

BLU-945 is a potent, highly selective, reversible, and orally bioavailable tyrosine kinase inhibitor (TKI) targeting mutant forms of the epidermal growth factor receptor (EGFR). It effectively inhibits EGFR variants harboring activating mutations such as L858R or exon 19 deletions, as well as resistance-associated mutations including T790M and C797S. BLU-945 is being developed as a next-generation therapeutic agent for the treatment of EGFR-mutant non-small cell lung cancer (NSCLC), particularly in cases resistant to earlier-generation EGFR inhibitors.

Cat. No.

A24035

CAS No.

1934259-00-3

Limertinib (ASK120067)

Synonyms: ASK120067

Limertinib (ASK120067) is a potent and orally active third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that selectively targets the EGFR^T790M resistance mutation with an IC₅₀ of 0.3 nM, while exhibiting reduced activity against wild-type EGFR (EGFR^WT, IC₅₀ = 6.0 nM). It is being investigated as a targeted therapy for non-small cell lung cancer (NSCLC) harboring EGFR-activating and resistance mutations.

Cat. No.

A24036

CAS No.

149092-50-2

AG-825 (Tyrphostin AG-825)

Synonyms: Tyrphostin AG-825

AG-825 is a selective, ATP-competitive inhibitor of ErbB2 (HER2) tyrosine kinase, with an IC₅₀ of 0.35 μM. It exhibits both anticancer and anti-inflammatory activities and has been shown to significantly accelerate apoptosis in human neutrophils. AG-825 also increases β₁-adrenergic receptor (β₁AR) density, suggesting potential cardiomodulatory effects. Due to its multifaceted biological activity, AG-825 is a valuable compound for research in oncology, inflammation, and cardiovascular disease.

Cat. No.

A24093

CAS No.

2772612-96-9

MS9449

MS9449 is a potent PROTAC-based degrader of the epidermal growth factor receptor (EGFR), exhibiting strong binding affinities with K\_d values of 17 nM for wild-type EGFR and 10 nM for the L858R mutant. It effectively induces degradation of mutant EGFR proteins via both the ubiquitin–proteasome system (UPS) and the autophagy–lysosome pathway, enabling dual-pathway clearance. MS9449 shows strong antiproliferative activity in non-small cell lung cancer (NSCLC) cells, making it a valuable compound for anticancer research, particularly in EGFR-driven tumors.

Cat. No.

A24099

CAS No.

2675490-92-1

MS39

MS-39 is a highly potent and selective PROTAC degrader specifically engineered to target mutant forms of the epidermal growth factor receptor (EGFR). It is constructed by conjugating the EGFR inhibitor gefitinib to a von Hippel–Lindau (VHL) E3 ligase ligand via a tailored linker. MS-39 exhibits strong binding affinity and efficient degradation of mutant EGFR proteins, offering a promising strategy for overcoming resistance in EGFR-driven cancers. Its design enables targeted proteasomal degradation rather than mere kinase inhibition, providing a novel approach to cancer therapy.

Cat. No.

A24121

CAS No.

102130-90-5

Isoprocurcumenol

Isoprocurcumenol is a guaiane-type sesquiterpene isolated from *Curcuma comosa* with notable bioactivity in epidermal growth factor receptor (EGFR) signaling. It activates EGFR and enhances downstream phosphorylation of ERK and AKT, key mediators of cell survival and proliferation pathways. As a result, isoprocurcumenol promotes keratinocyte proliferation, suggesting potential applications in skin regeneration, wound healing, and dermatological research.

Cat. No.

A24162

JBJ-09-063 hydrochloride

JBJ-09-063 hydrochloride is a highly potent, mutant-selective allosteric inhibitor of epidermal growth factor receptor (EGFR), specifically designed to target both TKI-sensitive and TKI-resistant EGFR mutations. It exhibits exceptionally low IC₅₀ values of: * 0.147 nM for EGFR L858R * 0.063 nM for EGFR L858R/T790M * 0.083 nM for EGFR L858R/T790M/C797S * 0.396 nM for EGFR^LT/L747S JBJ-09-063 hydrochloride effectively suppresses phosphorylation of EGFR and downstream signaling components, including Akt and ERK1/2, thereby inhibiting oncogenic signaling pathways. Its robust efficacy across a range of EGFR mutation profiles—including triple mutants that are resistant to third-generation TKIs—makes it a promising candidate for research and development in the treatment of EGFR-mutant non-small cell lung cancer (NSCLC).

Cat. No.

A24172

CAS No.

5334-30-5

PP 3

PP 3 (Compound 3) is an EGFR tyrosine kinase inhibitor with an IC50 of 2.7 μM. It targets the EGFR signaling pathway, which is critical for cell proliferation and survival in various cancers. PP 3 is a useful tool for research into EGFR-driven malignancies, such as non-small cell lung cancer and head and neck squamous cell carcinoma, enabling studies on tumor growth inhibition and potential therapeutic strategies.

Cat. No.

A24173

CAS No.

1042385-75-0

Dacomitinib hydrate

Synonyms: PF-00299804 hydrate; PF-299804 hydrate

Dacomitinib (PF-00299804) hydrate is an orally active, irreversible pan-ErbB inhibitor targeting EGFR, HER2, and HER4. It potently inhibits ErbB family signaling pathways, suppressing tumor proliferation and survival. Dacomitinib hydrate is a valuable agent for research into cancers, particularly metastatic non-small cell lung cancer (NSCLC), where it demonstrates efficacy in targeting EGFR-driven oncogenesis.

Cat. No.

A24174

CAS No.

1835667-12-3

Rezivertinib (BPI-7711)

Synonyms: BPI-7711

Rezivertinib (BPI-7711) is an orally active, highly selective, and irreversible third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI). It is designed to potently target both common activating EGFR mutations and the resistance-associated T790M mutation, which is a frequent cause of acquired resistance to earlier-generation TKIs. Rezivertinib also demonstrates excellent central nervous system (CNS) penetration, making it effective against brain metastases in EGFR-mutant non-small cell lung cancer (NSCLC). With its strong antitumor activity and favorable pharmacokinetic profile, Rezivertinib is a promising candidate for the treatment of EGFR-mutant NSCLC, particularly in patients with CNS involvement or T790M-driven resistance.

Cat. No.

A24175

CAS No.

2791417-66-6

MTX-531

MTX-531 is an orally active small molecule that inhibits EGFR (IC50 = 14.7 nM) and multiple PI3K isoforms, with IC50 values of 6.4 nM (PI3Kα), 233 nM (PI3Kβ), 8.3 nM (PI3Kγ), and 1.1 nM (PI3Kδ), demonstrating potent antitumor activity. Additionally, MTX-531 functions as a weak PPARγ agonist (IC50 = 2.5 µM), which may mitigate PI3K inhibitor-induced hyperglycemia.

Cat. No.

A24176

CAS No.

847949-49-9

O-Desmethyl gefitinib

O-Desmethyl gefitinib is an active plasma metabolite of gefitinib, formed via CYP2D6-mediated metabolism. It retains EGFR inhibitory activity with an IC50 of 36 nM in subcellular assays.

Cat. No.

A24177

CAS No.

2226167-02-6

Befotertinib mesylate (D-0316)

Synonyms: D-0316

Befotertinib (D-0316) mesylate is an orally active EGFR tyrosine kinase inhibitor that suppresses tumor cell proliferation. It is primarily investigated for its potential in treating EGFR T790M-positive non-small cell lung cancer (NSCLC).

Cat. No.

A24178

CAS No.

2607829-38-7

Silevertinib (BDTX-1535, EGFR-IN-76)

Synonyms: BDTX-1535; EGFR-IN-76

Silevertinib (BDTX-1535, EGFR-IN-76) is an orally bioavailable, blood-brain barrier-permeable, and selective EGFR inhibitor with demonstrated antitumor activity. It has shown efficacy in preclinical models of non-small cell lung cancer (NSCLC), glioblastoma patient-derived tumors, and intracranial tumor models.

Cat. No.

A24179

CAS No.

2260886-64-2

JND3229

JND3229 is a reversible EGFR C797S inhibitor with IC50 values of 5.8 nM for EGFR^L858R/T790M/C797S, 6.8 nM for EGFR^WT, and 30.5 nM for EGFR^L858R/T790M. It exhibits potent antiproliferative activity and effectively suppresses tumor growth in vivo, making it a valuable tool for cancer research, particularly in the context of non-small cell lung carcinoma.

Cat. No.

A24180

CAS No.

1557268-88-8

Avitinib maleate

Synonyms: Abivertinib maleate; AC0010 maleate

Avitinib (Abivertinib) maleate is a third-generation, irreversible, and orally active selective EGFR inhibitor with IC50 values of 0.18 nM for both EGFR^L858R and EGFR^T790M, and 7.68 nM for wild-type EGFR. In addition to its EGFR-targeting activity, Avitinib maleate also inhibits BTK phosphorylation and induces apoptosis in mantle cell lymphoma models, demonstrating broad-spectrum anticancer efficacy.

Cat. No.

A24183

CAS No.

592-95-0

Sulforaphene

Sulforaphene, a natural compound isolated from radish seeds, exhibits an ED₅₀ of approximately 2 × 10⁻⁴ M against velvetleaf seedlings. It promotes apoptosis and inhibits migration in cancer cells by suppressing signaling pathways including EGFR, phosphorylated ERK1/2 (p-ERK1/2), and NF-κB.

Cat. No.

A24194

CAS No.

1464910-32-4

JG26

JG26 is a potent ADAM inhibitor with IC50 values of 12 nM for ADAM8, 1.9 nM for ADAM17, and 150 nM for ADAM10. It also inhibits MMP-12 with an IC50 of 9.4 nM. JG26 suppresses AngII-induced EGFR transactivation and ERK activation, upregulates ACE2 expression, inhibits CD23 shedding, and reduces SARS-CoV-2 infection. Additionally, JG26 demonstrates anti-metastatic effects in colorectal cancer and holds research potential in Hodgkin lymphoma and vascular diseases.

Cat. No.

A24336

CAS No.

2728667-27-2

Zongertinib (BI 1810631)

Synonyms: BI 1810631

Zongertinib (BI 1810631) is a potent and selective tyrosine kinase inhibitor targeting HER2 and EGFR, with IC50 values of 13 nM and 579 nM, respectively. It exhibits significant antitumor activity and is being investigated for the treatment of multiple solid tumors, particularly those driven by HER2 alterations.

Cat. No.

A24846

CAS No.

2550393-21-8

MS154

MS154 is a novel E3 ligase cereblon-recruited degrader specifically targeting epidermal growth factor receptor (EGFR). It has demonstrated potent degradation of the EGFR L858R mutant in cancer cell lines with Kd values of 1.8 nM and 3.8 nM for wild-type and mutant EGFR, respectively. This selective degradation mechanism highlights its potential as an anticancer agent, particularly in lung cancer treatment. MS154 operates through an E3 ligase-dependent pathway, representing a promising therapeutic strategy for treating EGFR-driven malignancies.

Cat. No.

A25678

CAS No.

1373764-87-4

WB-308

WB-308 is a small molecule EGFR inhibitor, designed to target the epidermal growth factor receptor and its associated signaling pathways. In vitro studies demonstrate that WB-308 effectively reduces the proliferation and clonogenicity of non-small cell lung cancer (NSCLC) cells, leading to G2/M phase arrest and apoptosis. Additionally, it demonstrates tumor growth inhibition in both lung orthotopic transplantation and patient-derived xenograft models. WB-308 was shown to impair the phosphorylation of EGFR, AKT, and ERK1/2 proteins, offering a promising alternative to existing EGFR-targeted therapies with potentially lower cytotoxicity.

Cat. No.

A25693

CAS No.

129724-42-1

Melafolone

Melafolone is a potent dual inhibitor of COX-2 and EGFR, displaying IC50 values of 13.2 μM for COX-2 and 17.4 μM for EGFR. This compound enhances the efficacy of anti-PD-1 therapy by promoting vascular normalization and downregulating PD-L1 through the PI3K/Akt signaling pathway in Lewis lung carcinoma (LLC) and CMT167 models. Melafolone is suitable for applications in lung cancer research.

Cat. No.

A25694

CAS No.

2754394-10-8

EGFR-IN-176

EGFR-IN-176 is an orally active, ATP-competitive inhibitor specifically targeting mutant forms of the epidermal growth factor receptor (EGFR), notably the C797S-mediated triple mutant. This compound effectively suppresses AKT signaling pathways and induces apoptosis in Ba/F3 and PC-9 cell lines expressing the EGFR mutations EGFR19del/T790M/C797S and EGFRL858R/T790M/C797S. Selectivity is demonstrated by its lack of inhibition against wild-type EGFR-expressing A431 cells. Additionally, EGFR-IN-176 inhibits ALK enzymatic activity with an IC50 of less than 0.5 nM and serves as a valuable tool for research in non-small cell lung cancer (NSCLC).

Cat. No.

A25699

CAS No.

1260401-93-1

KU004

KU004 is a potent dual inhibitor of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), exhibiting significant anticancer properties. This quinazoline derivative effectively inhibits the proliferation of human breast cancer SKBR3 cells through the induction of G1 phase cell cycle arrest. KU004 interferes with HER2 and EGFR activation, subsequently blocking downstream signaling pathways such as Akt and Erk, and promotes apoptosis primarily via the extrinsic pathway. Its mechanism makes it a valuable tool for cancer research, particularly in studies targeting breast cancer therapy.

Cat. No.

A25741

CAS No.

3081622-35-4

EGFR kinase-IN-8

EGFR kinase-IN-8 is a potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating strong inhibitory activity against both triple-mutated EGFR (L858R/T790M/C797S) and double-mutated EGFR (L858R/T790M), with IC50 values of 3.86 nM and 1.23 nM, respectively. This compound effectively suppresses EGFR phosphorylation, leading to inhibition of downstream signaling pathways, including AKT, STAT3, and MAPK. EGFR kinase-IN-8 has shown promising anticancer efficacy, particularly in the treatment of non-small cell lung cancer.