EGFR Inhibitor

Rociletinib hydrobromide (Standard) is the analytical standard of Rociletinib hydrobromide. This product is intended for research and analytical applications. Rociletinib hydrobromide (CO-1686 hydrobromide) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.

AKOS024836912 is a EGFR-EGF interaction inhibitor. AKOS024836912 is applicable to research related to non-small cell lung cancer.

Icotinib (Standard) is the analytical standard of Icotinib. This product is intended for research and analytical applications. Icotinib (BPI-2009) is a potent and specific EGFR inhibitor with an IC₅₀ of 5 nM; also inhibits mutant EGFR^L858R, EGFR^L858R/T790M, EGFR^T790M and EGFR^L861Q. Icotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Tyrphostin 23 (Standard) is the analytical standard of Tyrphostin 23. This product is intended for research and analytical applications. Tyrphostin 23 (Tyrphostin A23) is an EGFR inhibitor with an IC50 and Kiof 35 and 11 μM, respectively.

ZM-306416 (CB-676475) hydrochloride is a potent VEGFR inhibitor with IC₅₀s of 0.1 μM and 2 μM for KDR and Flt, respectively. ZM-306416 hydrochloride is also a EGFR inhibitor with an IC₅₀ of <10 nM.

Paeciloquinone C can inhibit the EGFR protein tyrosine kinase. Paeciloquinone C inhibits the V-abl protein tyrosine K_inase with an IC₅₀ of 0.56 μM.

MTX-211 (Standard) (Mol 211 (Standard)) is the analytical standard of MTX-211 (HY-107364). This product is intended for research and analytical applications. MTX-211 (Mol 211) is a dual inhibitor of EGFR and PI3K with IC₅₀ values of ＜100 nM. MTX-211 can be used for the research of cancer and other diseases.

TX1-85-1 (Standard) is the analytical standard of TX1-85-1 (HY-100848). This product is intended for research and analytical applications. TX1-85-1 is an irreversible Her3 (ErbB3) inhibitor with an IC50 of 23 nM. TX1-85-1 is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3. TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling.

1,2,3,4-Tetrahydrostaurosporine is a derivative of Staurosporine (HY-15141) and an inhibitor of mutant EGFR (IC₅₀=74 nM for EGFRT790M). It is selective for EGFRT790M over wild-type EGFR (IC₅₀=390 nM). It also binds to Janus kinase 3 (JAK3).

Rezivertinib (Standard) is the analytical standard of Rezivertinib (HY-109189). This product is intended for research and analytical applications. Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine K_inase inhibitor (TK_i). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity.

Pelitinib (Standard) is the analytical standard of Pelitinib. This product is intended for research and analytical applications. Pelitinib (EKB-569;WAY-EKB 569) is an irreversible inhibitor of EGFR with an IC50 of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282, 800, and 1255 nM, respectively.

HKI-357 (Standard) is the analytical standard of HKI-357 (HY-103443). This product is intended for research and analytical applications. HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC₅₀s of 34 nM and 33 nM, respectively. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation.

CNBDA is a selective SHP2 inhibitor with an IC₅₀ of 5 μM. CNBDA binds to the active site of SHP2 through interactions with surrounding positively charged and polar amino acids, inhibits the PTPase activity of SHP2, and blocks the autodephosphorylation of SHP2. CNBDA inhibits the transformed phenotype, proliferation, anchorage-independent growth, and mammosphere formation of breast cancer cells, as well as EGF-induced Ras-ERK and PI3K-Akt signaling pathways, downregulates HER2 expression, and induces cell death. CNBDA can be used in breast cancer-related research.

BMS-690514 (Standard) is the analytical standard of BMS-690514 (HY-10333). This product is intended for research and analytical applications. BMS-690514 is a potent and orally active inhibitor of EGFR and VEGFR; has IC₅₀s of 5, 20 and 60 nM for EGFR, HER 2 and HER 4, respectively.

Tucatinib-d₆ (Irbinitinib-d₆) is deuterium labeled Tucatinib. Tucatinib (Irbinitinib) is a potent, orally active and selective HER2 inhibitor with an IC₅₀ of 8 nM.

Erlotinib-d₄ (CP-358774-d₄) is the deuterated-labeled Erlotinib (HY-50896). Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib also acts as a substrate and inhibitor of OATP2B1, with an IC₅₀ of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, fibronectin, α-SMA, collagen deposition, and renal injury markers. Erlotinib is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, pancreatic cancer, renal fibrosis, and other conditions.

4(3H) -quinazolinone is a fused nitrogen heterocyclic compound whose derivatives have a wide range of antimicrobial and antitumor activities.

Lapatinib-d₇ (GW572016-d₇) 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.

Trastuzumab envedotin (DP303c) is a anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab envedotin is composed of the tubulin polymerization inhibitor Monomethyl auristatin E (MMAE) (HY-15162) to the anti-HER2 antibody DP001 via a cleavable linker. Trastuzumab envedotin can be used for the research of HER2-positive solid tumors, such as breast cancer, colorectal cancer, and gastric cancer.

LDC8201 is a selective, orally active, covalent inhibitor that targets EGFR and Her2 exon 20 insertion mutants. LDC8201 induces tumor shrinkage and regression. LDC8201 is applicable to research related to non-small cell lung cancer carrying EGFR or Her2 exon 20 insertion mutations.