EGFR Inhibitor

Canertinib (dihydrochloride) (Standard) is the analytical standard of Canertinib (dihydrochloride). This product is intended for research and analytical applications. Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM. Canertinib dihydrochloride is active against vaccinia virus respiratory infection in mice.

HKI-357 dimaleate is an irreversible dual inhibitor of EGFR and ERBB2 with IC₅₀s of 34 nM and 33 nM, respectively. HKI-357 dimaleate suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation.

(E/Z)-Afatinib (Standard) is the analytical standard of (E/Z)-Afatinib. This product is intended for research and analytical applications. (E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells.

GI261520A is a egfr/erbb2 dual inhibitor. GI261520A inhibits PhoQ phosphorylation dose-dependently. GI261520A can downregulate the activity levels of PhoP/PhoQ. GI261520A inhibits pagC reporter expression levels with an IC₅₀ of 3.2 μM. GI261520A inhibits PhoQc autokinase activtiy by 80%. GI261520A can permeate the eukaryotic plasmatic and vascular cell membranes and reach intravacuolar Salmonella to block intramacrophage proliferation.

AG490 (Standard) is the analytical standard of AG490 (HY-12000). This product is intended for research and analytical applications. AG490 (Tyrphostin AG490) is a tyrosine K_inase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.

Lapatinib (ditosylate) (Standard) is the analytical standard of Lapatinib (ditosylate). This product is intended for research and analytical applications. Lapatinib ditosylate (GW572016 ditosylate) 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.

Mobocertinib (Standard) is the analytical standard of Mobocertinib. This product is intended for research and analytical applications. Mobocertinib (TAK-788) is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib can be used in NSCLC research.

Neratinib-d₆ (HKI-272-d6) is the deuterium labeled Neratinib. Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor with IC50s of 59 nM and 92 nM for HER2 and EGFR, respectively.

AEE788 (Standard) is the analytical standard of AEE788 (HY-10045). This product is intended for research and analytical applications. AEE788 is an inhibitor of the EGFR and ErbB2 with IC50 values of 2 and 6 nM, respectively.

Dacomitinib (Standard) is the analytical standard of Dacomitinib. This product is intended for research and analytical applications. Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC₅₀s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.

Canertinib (Standard) is the analytical standard of Canertinib. This product is intended for research and analytical applications. Canertinib (CI-1033;PD-183805) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM. Canertinib is active against vaccinia virus respiratory infection in mice.

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.

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.