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HER2
| Cat. No. | Product Name | CAS No. | Information |
|---|---|---|---|
| CSN16336 | XL647 | 781613-23-8 | XL647 or tesevatinib inhibits EGFR, HER2, VEGFR and EphB4 with potential antineoplastic activity. |
| CSN16032 | Varlitinib | 845272-21-1 | Varlitinib is a selective and potent ErbB1 EGFR and ErbB2 HER2 inhibitor with IC50 of 7 nM and 2 nM respectively |
| CSN12170 | Tyrphostin AG 879 | 148741-30-4 | Tyrphostin AG 879 potently inhibits HER2ErbB2 with IC50 of 1 M 100- and 500-fold higher selective to ErbB2 than PDGFR and EGFR |
| CSN26545 | Tarloxotinib bromide | 1636180-98-7 | Tarloxotinib bromide, also known TH-4000 or PR-610, is a prodrug designed to selectively release a covalent (irreversible) EGFR tyrosine kinase inhibitor under severe hypoxia, a feature of many solid tumors. Tarloxotinib has the potential to effectively shut down aberrant EGFR signaling in a tumor-selective manner, thus potentially avoiding or reducing the systemic side effects associated with currently available EGFR tyrosine kinase inhibitors. |
| CSN26124 | Mobocertinib | 1847461-43-1 | TAK-788 is an investigational TKI with potent, selective preclinical activity against activating EGFR and HER2 mutations, including exon 20 insertions. It is in a phase 1/2 open-label, multicenter study. |
| CSN16247 | TAK-285 | 871026-44-7 | TAK-285 is a dual HER2 and EGFR HER1 inhibitor with IC50 of 17 nM and 23 nM 10-fold selectivity for HER12 than HER4 less potent to MEK15 c-Met Aurora B Lck CSK etc |
| CSN16204 | Poziotinib | 1092364-38-9 | Poziotinib is an irreversible Pan-HER inhibitor with IC50s of 3/5/23 nM for HER1/HER2/HER4 respectively. |
| CSN20576 | Neratinib Maleate | 915942-22-2 | Neratinib maleate is an orally available irreversible tyrosine kinase inhibitor with IC50 of 59 nM and 92 nM for HER2 and EGFR respectively |
| CSN12420 | Neratinib | 698387-09-6 | Neratinib is an orally available irreversible tyrosine kinase inhibitor with IC50 of 59 nM and 92 nM for HER2 and EGFR respectively |
| CSN11482 | Mubritinib | 366017-09-6 | Mubritinib is a potent and selective inhibitor of HER2ErbB2 with IC50 of 6 nM with no inhibition on EGFR FGFR PDGFR and etc |
| CSN27281 | Mobocertinib succinate | 2389149-74-8 | Mobocertinib succinate is an inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. |
| CSN11269 | Lapatinib Ditosylate | 388082-77-7 | Lapatinib ditosylate is a potent EGFR and ErbB2 inhibitor with IC50 of 108 and 92 nM respectively |
| CSN18606 | Irbinitinib | 937263-43-9 | Irbinitinib is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold selective for HER2 versus EGFR. |
| CSN13899 | Dacomitinib | 1110813-31-4 | Dacomitinib is a potent, orally available, irreversible tyrosine kinase HER 1 (EGFR), HER2 and HER4 inhibitor with IC50 of 6, 45.7 and 73.7 nM for EGFR, ERBB2 and ERBB4, respectively. |
| CSN12702 | CP-724714 (Random Configuration) | 537705-08-1 | CP-724714 is a potent selective inhibitor of HER2ErbB2 with IC50 of 10 nM 640-fold selectivity against EGFR InsR IRG-1R PDGFR VEGFR2 Abl Src c-Met etc in cell-free assays |
| CSN18252 | CP-724714 | 383432-38-0 | CP-724714 is a potent selective inhibitor of HER2ErbB2 with IC50 of 10 nM 640-fold selectivity against EGFR InsR IRG-1R PDGFR VEGFR2 Abl Src c-Met etc |
| CSN10535 | Canertinib 2HCl | 289499-45-2 | Canertinib 2HCl, an irreversible quinazoline-based HER family tyrosine kinase inhibitor, inhibits EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM respectively. Phase II. |
| CSN18515 | BMS-599626 HCl | 873837-23-1 | BMS-599626 is an inhibitor of HER1 IC50 20 nM and HER2 IC50 30 nM |
| CSN15811 | AZD8931 | 848942-61-0 | AZD8931 is a reversible, ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4 nM, 3 nM and 4 nM respectively. |
| CSN18835 | AST-1306 p-Toluenesulfonic Acid | 1050500-29-2 | AST-1306 p-toluenesulfonic acid is an irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790ML858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases. |
| CSN16578 | AST-1306 | 897383-62-9 | AST-1306 is an irreversible inhibitor of EGFR and ErbB2 with IC50 of 05 nM and 3 nM also effective in mutation EGFR T790ML858R more potent to ErbB2-overexpressing cells 3000-fold selective for ErbB family than other kinases |
| CSN17153 | ARRY-380 Analog | 937265-83-3 | ARRY-380 analog is a potent and selective HER2 inhibitor with IC50 of 8 nM equipotent against truncated p95-HER2 500-fold selective for HER2 versus EGFR |
| CSN12703 | Afatinib | 850140-72-6 | Afatinib E-isomer is an irreversible inhibitor of dual EGFR and HER2 that shows obvious activitives of EGFR wt EGFR L858R EGFR L858RT790M and HER2 with IC50 of 05 nM 04 nM 10 nM and 14 nM respectively |
| CSN12809 | AC480 | 714971-09-2 | AC480 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 |
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