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Inhibitors
| Cat.No. | Name | Information |
|---|---|---|
| M9535 | Mobocertinib | Mobocertinib (TAK-788) is an investigational TKI with potent, selective preclinical activity against activating EGFR and HER2 mutations, including exon 20 insertions. |
| M9534 | TAS6417 | TAS6417 is a novel EGFR inhibitor targeting exon 20 insertion mutations, with IC50 values range from 1.1-8.0 nM. |
| M9400 | AST2818 mesylate | AST2818 mesylate is a third generation EGFR inhibitor that targets both EGFR activating mutations and T790M thus leading to tumor growth inhibition. |
| M9132 | ABM-3627 | ABM-3627, also known as Mutant EGFR inhibitor, is a selective and potent Mutated EGFR 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 an allosteric inhibitor that targets selected drug-resistant EGFR mutants but spares the wild-type receptor. |
| 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 | CH5183284 | 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 new antihistamine with peripheral HI-antagonist potency equal to that of triprolidine, but in doses up to 4 mg acrivastine does not impair performance on a vigilance task or increase. 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 | AZD-9291 (Mesylate) | AZD-9291 is a potent and selective mutated forms EGFR inhibitor(Exon 19 deletion EGFR IC50=12.92 nM, L858R/T790M EGFR IC50= 11.44 nM, wild type EGFR IC50= 493.8 nM). |
| 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. |
| M4850 | PD153035 | PD153035 is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM. |
| M4805 | BIBX 1382 | BIBX 1382 is a potent, selective inhibitor of EGFR tyrosine kinase (IC50 = 3 nM); displays > 1000-fold lower potency against ErbB2 (IC50 = 3.4 μM) and a range of other related tyrosine kinases (IC50 > 10 μM). |
| M4585 | Taxifolin | Taxifolin, type I inhibitor for VEGFR-2 kinase, is a flavonoid in many plants such as Taxus chinensis, Siberian larch, Cedrus deodara and so on. |
| M4208 | (-)-Epigallocatechin gallate | (-)-Epigallocatechin Gallate is an antioxidant polyphenol flavonoid form green tea, and inhibits the activation of EGFR, HER2 and HER3, with antitumor activity. |
| M4002 | Chrysophanic acid | Chrysophanic acid, also known as chrysophanol, is a fungal isolate and a natural anthraquinone with anti-cancer activity. |
| M3780 | XL647 | XL647 is an extremely potent and selective inhibitor of EGFR phosphorylation (IC50 = 0.3 nM). |
| M3689 | PD153035 hydrochloride | PD153035 hydrochloride is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM. |
| M3684 | Canertinib dihydrochloride | Canertinib 2HCl is a pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, no activity to PDGFR, FGFR, InsR, PKC, or CDK1/2/4. |
| M3569 | AST-1306 | AST-1306 is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases, |
| M3560 | ARRY-380 | ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold more selective for HER2 versus EGFR. |
| M3553 | TAK-285 | TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. |
| 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. |
| M3491 | OSI-420 | OSI-420 is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM). |
| M3238 | 4-Quinazolinamine | 4-Quinazolinamine (4-Aminoquinazoline) is a potent and highly selective EGFR tyrosine kinase inhibitor. |
| M3217 | AV-412 | AV-412 is a second-generation, orally bioavailable dual EGFR/HER2 tyrosine kinase inhibitor. |
| M3199 | Varlitinib | ARRY334543 is a selective and potent ErbB1(EGFR) and ErbB2(HER2) inhibitor with IC50 of 7 nM and 2 nM, respectively. |
| M3098 | AG 879 | Tyrphostin AG 879 potently inhibits HER2/ErbB2 with IC50 of 1 μM, 100- and 500-fold higher selective to ErbB2 than PDGFR and EGFR. |
| M2916 | PD168393 | PD168393 is an irreversible EGFR inhibitor with IC50 of 0.70 nM, irreversibly alkylate Cys-773; inactive against insulin, PDGFR, FGFR and PKC. |
| M2464 | BMS-690514 | BMS-690514 is a potent inhibitor of EGFR and VEGFR2 with IC50 of 5 nM and 50 nM, respectively. |
| M2424 | AZD9291 | AZD9291 is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR, respectively. |
| M2312 | AG-1478 | AG-1478 (Tyrphostin AG-1478) is a selective EGFR inhibitor with IC50 of 3 nM. |
| M2255 | Genistein | Genistein is a highly specific inhibitor of protein tyrosine kinase (PTK) which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells with IC50 of 12μM or by insulin with IC50 of 19 μM. |
| M2212 | CO-1686 | CO-1686 is a potent, novel inhibitor of EGFR L858R/T790M kinase with Ki of 21.5 nM and 303.3 nM, respectively. |
| M2117 | CNX-2006 | CNX-2006 is a novel irreversible EGFR inhibitor with IC50 value of <20 nM. |
| M2021 | AG 18 | AG-18 is an inhibitor of EGF receptor kinase with an IC50 value of 35 μM. |
| M1943 | Canertinib | Canertinib (CI-1033) is an irreversible tyrosine-kinase inhibitor with activity against EGFR (IC50 0.8 nM), HER-2 (IC50 19 nM) and ErbB-4 (IC50 7 nM). |
| M1919 | Mubritinib | Mubritinib (TAK-165) is a new potent inhibitor of human epidermal growth factor receptor 2 (HER2) tyrosine kinase (IC50 = 6 nM). |
| M1913 | Neratinib | Neratinib (HKI-272) is an orally available, irreversible inhibitor of Her 2 tyrosine kinase. |
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