EGFR Inhibitor

EGFR Inhibitors (1003):

Cat. No.	Nom du produit	Effet	Pureté

HY-112823S

Almonertinib-d₆	Inhibitor
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.

HY-157994

EGFR WT/T790M-IN-2	Inhibitor
EGFR WT/T790M-IN-2 (Compound 7c) is a EGFR T790M/WT inhibitor with IC₅₀ values of 0.08 and 0.13 μM, respectively. EGFR WT/T790M-IN-2 induces apoptosis by blocking the G0-G1 phase (apoptosis). EGFR WT/T790M-IN-2 has antitumor activity.

HY-168433

LSD1/EGFR-IN-1	Inhibitor
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.

HY-184116

A2AR/EGFR-IN-1	Inhibitor
A2AR/EGFR-IN-1 is a dual A2AR/EGFR inhibitor, with an IC₅₀ of 0.037 μM against A2AR and an IC₅₀ of 8.37 μM against EGFR. A2AR/EGFR-IN-1 induces cell cycle arrest at S and G2/M phases. A2AR/EGFR-IN-1 upregulates the expression of TP53, Caspase3 and Bax, downregulates the expression of Bcl2, and promotes cell Apoptosis. A2AR/EGFR-IN-1 restores colon crypt structure in an azoxymethane (HY-111375)-induced colorectal cancer model in vivo. A2AR/EGFR-IN-1 can be used for research related to colorectal cancer.

HY-147967

EGFR-IN-63	Inhibitor
EGFR-IN-63 is an EGFR inhibition (IC₅₀: 0.096 μM) and it has anticancer activity in MCF-7 cells (IC₅₀: 2.49 μM).

HY-149517

EGFR/BRAFV600E-IN-2	Inhibitor
EGFR/BRAFV600E-IN-2 (compound 3g) is a potential multi-target inhibitor of EGFR, BRAF^V600E, and EGFR^T790M, and an inducer of apoptosis. EGFR/BRAFV600E-IN-2 can activate caspase-3, 8, and Bax, and downregulate the anti-apoptotic protein Bcl2, inducing apoptosis. EGFR/BRAF V600E-IN-2 also has antioxidant activity and DPPH free radical scavenging potency.

HY-157399

EGFR/HER2-IN-10	Inhibitor
EGFR/HER2-IN-10 (compound 9F) is a potent and selective dual EGFR/HER2 inhibitor with IC₅₀s of 2.3 nM and 234 nM for EGFR and HER2, respectively. EGFR/HER2-IN-10 shows an effective antiproliferative action against prostate carcinoma.

HY-176938

AfaPhos1	Inhibitor
AfaPhos1 is a new, Afatinib (HY-10261)-based EGFR PhosTAC. AfaPhos1 induces EGFR dephosphorylation at both pY1068 and pY845. AfaPhos1 induces Apoptosis. AfaPhos1 has anticancer activity against non-small cell lung cancer.

HY-181766

EGFR/VEGFR2-IN-11	Inhibitor
EGFR/VEGFR2-IN-11 is an EGFR/VEGFR2 inhibitor with IC₅₀ values of 0.62 μM (human EGFR), 2.26 μM (human VEGFR-2), 17.38 μM (human COX-2), and 19.31 μM (human tubulin). EGFR/VEGFR2-IN-11 inhibits COX-2 activity and tubulin polymerization. EGFR/VEGFR2-IN-11 induces cell cycle arrest and apoptosis. EGFR/VEGFR2-IN-11 exerts selective and antiproliferative activity against human cancer cells. EGFR/VEGFR2-IN-11 can be used for the research of colon carcinoma, breast carcinoma, leukemia, lymphoma, glioblastoma.

HY-158969

EGFR-IN-113	Inhibitor
EGFR-IN-113 (compound II-1) is an EGFR kinase inhibitor with an IC₅₀ of 14.79 μM. EGFR-IN-113 can induce apoptosis and inhibit cell proliferation by downregulating Akt and Erk1/2 signaling. EGFR-IN-113 can be used for research in EGFR-driven cancers, such as lung cancer, pancreatic cancer, and breast cancer.

HY-147826

EGFR-IN-60	Inhibitor
EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFR^WT, EGFR^T790M, EGFR^L858R and JAK3 with IC₅₀s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFR^T790M mutation (IC₅₀=1.32 µM) over A431 cells overexpressing EGFR^WT (IC₅₀=4.96 µM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio.

HY-P10793

Cyclic(YCDGFYACYMDV)	Inhibitor
Cyclic(YCDGFYACYMDV) is a HER2 signaling pathway inhibitor with anti-cancer activity. This compound self-assembles into nanoparticles in aqueous solution and transforms into nanofibers upon specific binding to HER2 on cancer cells. This transformation disrupts HER2 dimerization and subsequent downstream signaling events, leading to cancer cell apoptosis (Apoptosis). The inhibitory effects on HER2 positive breast cancer have been demonstrated to be effective in a murine xenograft model.

HY-175608

EGFR-IN-171	Inhibitor
EGFR-IN-171 is an EGFR inhibitor with an IC₅₀ value of 0.19 μM. EGFR-IN-171 also inhibits vascular endothelial growth factor 2 (VEGFR-2) with an IC₅₀ value of 31.65 μM. EGFR-IN-171 can induce apoptosis and G2/M phase cell cycle arrest. EGFR-IN-171 can be used for cancer research, such as liver and breast cancer.

HY-13050A

Sapitinib fumarate	Inhibitor
Sapitinib fumarate is a reversible, ATP competitive EGFR inhibitor of with IC₅₀s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.

HY-153744

JGK-068S	Inhibitor
JGK-068S (compound I) is a potent EGFR inhibitor.

HY-175257

Theophylline-platinum(IV) prodrug-1	Inhibitor
Theophylline-platinum(IV) prodrug-1 is a PARP-1 inhibitor. Theophylline-platinum(IV) prodrug-1 enhances DNA damage, ROS production, mitochondrial dysfunction, apoptosis and S-phase arrest, along with reducing invasion and metastasis in cells. Theophylline-platinum(IV) prodrug-1 exhibits superior antitumor activity in the xenograft SKOV3-BRCA1-KD tumor model. Theophylline-platinum(IV) prodrug-1 can be used for the study of ovarian cancer.

HY-178448

EGFR-IN-178	Inhibitor
EGFR-IN-178 is an orally active EGFR mutant inhibitor, exhibits highly selective inhibitory activity against mutants of the EGFR enzyme, including Del19 (IC₅₀ = 3.4 nM), L858R/T790 M (IC₅₀ = 2.9 nM), and Del19/T790 M (IC₅₀ = 2.5 nM). EGFR-IN-178 has good activity against JAK2 (IC₅₀ = 55.6 nM) and JAK3 (IC₅₀ = 46.1 nM) kinases. EGFR-IN-178 can increase cellular lipid oxide MDA, meanwhile decrease GSH content, causing ferroptosis in cancer cells. EGFR-IN-178 promotes apoptosis by increasing cleaved caspase-3 expression. EGFR-IN-178 can inhibit the phosphorylation of EGFR protein and decrease the active form p-JAK2 for JAK2, induce an increase in intracellular ROS. EGFR-IN-178 can be used for the study of non-small cell lung cancer (NSCLC).

HY-158175

EGFR T790M/L858R-IN-4	Inhibitor
EGFR T790M/L858R-IN-4 (Example 14) is a potent EGFR^T790M/L858R inhibitor with anticancer effects.

HY-173492

EGFR-IN-156	Inhibitor
EGFR-IN-156 (Compound 7f) is an EGFR inhibitor that also has inhibitory activity against mutations EGFRL858R and EGFRT790M (IC₅₀ values are 0.186, 0.131, and 0.107 μM, respectively). EGFR-IN-156 has significant anticancer activity against human cancer cell lines HepG-29 (liver cancer), MCF-7 (breast cancer), and HCT-116 (colon cancer) (IC₅₀ values are 1.67, 5.32, and 6.56 μM, respectively). EGFR-IN-156 inhibits cancer cell proliferation by inducing cell cycle arrest at the G/G1 phase and triggering apoptosis. EGFR-IN-156 shows promise in EGFR-related cancers.

HY-147862

EGFR-IN-62	Inhibitor
EGFR-IN-62 (compound 9h) is a potent and reversible EGFR kinase inhibitor, with IC₅₀ values of 10 nM (L858R/T790 M), 29 nM (WT), and 242 nM (L858R/T790 M/C797S), respectively. EGFR-IN-62 shows antiproliferative activity against A549 and H1975 cell lines, with IC₅₀ values of 2.53 and 1.56 μM, respectively. EGFR-IN-62 induces dose-dependent apoptosis process, G1/G0-phase arrestation, and the inhibition of motility on A549 and/or H1975 cell lines.

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