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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. |
| M9132 | ABM-3627 | ABM-3627, also known as Mutant EGFR inhibitor, is a selective and potent Mutated EGFR inhibitor. |
| M8818 | Tyrphostin RG 13022 | RG13022 is a non-phenolic tyrphostin-class tyrosine kinase inhibitor. |
| M6411 | AG 494 | AG 494 is a potent EGFR-kinase inhibitor with an IC50 value of 1 µM in HT-22 cells. |
| M6221 | Pertuzumab | Pertuzumab, a humanized monoclonal antibody and the first in the class of agents called the HER2 dimerization inhibitors, impairs the ability of HER2 to bind to other members of the HER family, MW: 148 KD. |
| M6218 | Trastuzumab | Trastuzumab is a humanized, recombinant monoclonal antibody that binds to the extracellular domain of HER2, MW:145.53 KD. |
| M6103 | Cetuximab | Cetuximab, a novel molecular-targeted agent,is an inhibitor of EGFR monoclonal humanized antibody interacting with the extracellular binding site of EGFR to block ligand stimulation. |
| M6081 | EAI045 | EAI045 is a fourth generation allosteric inhibitor of mutant EGFR, which inhibits EGFR at 10 μM ATP, EGFRL858R, EGFRT790M and EGFRL858R/T790M with IC50 values of 1.9, 0.019, 0.19 and 0.002 μM respectively. |
| M5679 | Gefitinib HCl | Gefitinib Hcl(ZD-1839 Hcl) is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. Therefore, it is only effective in cancers with mutated and overactive EGFR. |
| 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. |
| M5346 | WZ3146 | WZ3146 is a mutant-selective irreversible inhibitor of EGFR(L858R) and EGFR(E746_A750) with IC50 of 2 nM and 2 nM; does not inhibit ERBB2 phosphorylation (T798I). |
| M5318 | Zoligratinib | CH5183284 is a selective and orally available FGFR inhibitor with IC50 of 9.3 nM, 7.6 nM, 22 nM, and 290 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. Phase 1. |
| M5307 | Afatinib dimaleate | Afatinib (BIBW2992) Dimaleate irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant. |
| M5286 | Acrivastine | Acrivastine is a novel antihistamine compound whose peripheral Hi-antagonist has the same potency as trichloropyridine, but doses of up to 4mg of atorvastatin do not reduce alert performance or increase response time. reaction time. |
| M5275 | Nazartinib | Nazartinib (EGF816, NVS-816) is a covalent, irreversible, mutant-selective EGFR inhibitor that has nanomolar inhibitory potency against activating mt (L858R, ex19del) and T790M mt, with up to 60-fold selectivity over wild type (wt) EGFR in vitro. |
| M5164 | AZD3759 | AZD3759 is a potent, oral active, CNS-penetrant EGFR inhibitor with IC50 of 0.3 nM, 0.2 nM, and 0.2 nM for EGFR (WT), EGFR (L858R), and EGFR (exon 19Del), respectively. |
| M5133 | Olmutinib | Olmutinib is a potent small molecule inhibitor of Bruton's tyrosine kinase (BTK). |
| M5127 | FIIN-2 | FIIN-2 is an irreversible, pan-FGFR inhibitor with IC50 of 3.09 nM, 4.3 nM, 27 nM and 45.3 nM for FGFR1/2/3/4, respectively. |
| M5099 | Osimertinib mesylate (AZD-9291 mesylate) | Osimertinib mesylate (AZD-9291 mesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively. |
| M5031 | Poziotinib | Poziotinib (NOV120101; HM781-36B) is an irreversible Pan-HER inhibitor with IC50s of 3/5/23 nM for HER1/HER2/HER4 respectively. |
| M4871 | CL-387785 | CL-387785 (EKI-785) is an irreversible, and selective EGFR inhibitor with IC50 of 370 pM. |
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