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EGFR/HER2 Epidermal growth factor receptor/Human epidermal growth factor receptor-2

Inhibitors

Cat.No.  Name Information
M3517 Lapatinib Lapatinib, used in the form of Lapatinib ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM, respectively.
M1802 Lapatinib Ditosylate Lapatinib Ditosylate (CAS 388082-78-8) is a selective and effective inhibitor of EGFR kinase (Ki = 3 nM), ErbB-2 kinase (Ki = 13 nM) and ErbB-4 kinase (Ki = 347 nM).
M1749 Gefitinib Gefitinib (ZD1839) is an EGFR tyrosine kinase and Akt phosphorylation inhibitor. Gefitinib significantly down-regulates CD47 expression and increases DC phagocytosis in non-small cell lung cancer cells such as PC9, H1437 and H1573. Gefitinib combined with CD47 antibody can enhance the phagocytosis of macrophages.
M5621 Erlotinib Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
M1913 Neratinib Neratinib (HKI-272) is an orally available, irreversible inhibitor of Her 2 tyrosine kinase.
M21108 Dosimertinib Dosimertinib is a highly potent, selective, orally effective EGFR inhibitor for the study of non-small cell lung cancer.
M21081 JBJ-09-063 JBJ-09-063 is an oral allogenic epidermal growth factor inhibitor currently in preclinical development for the study of non-small cell lung cancer (NSCLC) with epidermal growth factor L858R mutations.
M21051 BI-4142 BI-4142 is a HER2 exon 20 insertion mutant inhibitor being developed for non-small cell lung cancer (NSCLC), The IC50 value was 5 nM.
M20803 BDTX-189 BDTX-189 is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations with Kd of 0.2 nM, 0.76 nM, 13 nM and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. BDTX-189 exhibits anticancer activity.
M20622 Naquotinib(ASP8273) Naquotinib(ASP8273) is an orally available, irreversible, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity.
M20583 AG 555 AG-555 is an inhibitor of tyrosine kinase , interacts directly with topoisomerase I, thus preventing DNA relaxation. It inhibits EGFR with an IC50 of 0.7 μM.
M20388 AC480 (BMS-599626) AC480 (BMS-599626) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc. Phase 1.
M20314 WAY-312484 WAY-312484 is a EGFR inhibitor.
M20282 WAY-660222 WAY-660222 is a EGFR kinase inhibitor
M20264 WAY-647802 WAY-647802 is a EGFR or/and ALK inhibitor
M20168 WAY-354890 WAY-354890 is a EGFR kinase inhibitor.
M20147 WAY-339696 WAY-339696 is a inhibitor for EGFR-T790M/L858R.
M20092 WAY-321002 WAY-321002 is a EGFR inhibitor
M20023 GI-566508 GI-566508 is a EGFR kinase inhibitor.
M14142 Tucatinib hemiethanolate Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.
M14141 Tephrosin Tephrosin is a natural rotenoid which has potent antitumor activities. Tephrosin induces degradation of of EGFR and ErbB2 by inducing internalization of the receptors.
M14140 Pyrotinib dimaleate Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively.
M14139 Naquotinib mesylate Naquotinib mesylate (ASP8273 mesylate) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
M14138 Mobocertinib succinate Mobocertinib succinate (TAK-788 succinate) is a potent and orally active inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. Antitumor activity.
M14137 Lapatinib ditosylate Lapatinib ditosylate (GW572016 ditosylate) is a potent 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.



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