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HER2

HER2

货号 产品名 CAS号 信息
CSN16336 Tesevatinib 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 HER2/ErbB2 with IC50 of 1 μM, 100- and 500-fold higher selective to ErbB2 than PDGFR and EGFR.
CSN14056 Tephrosin 76-80-2 Tephrosin, a natural product isolated and purified from the herbs of Derris robusta, may be valuable for augmenting the therapeutic efficacy of 2-Deoxy-D-glucose(DG), has potent antitumor activity by inducing autophagy pathway, internalization and degradation of inactivated EGFR and ErbB2, and exerts antitumor effects by inducing internalization and degradation of inactivated EGFR and ErbB2 in human colon cancer cells.
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 HER1/2 than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc.
CSN20157 Pyrotinib 1269662-73-8 Pyrotinib is an irreversible pan-ErbB receptor tyrosine kinase inhibitor, in patients with HER2-Positive metastatic breast cancer.
CSN16204 Poziotinib (HM781-36B) 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 HER2/ErbB2 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 10.8 and 9.2 nM, respectively.
CSN18606 Tucatinib 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.
CSN25718 N-{3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl}-6-(2-{[(2-methanesulfonylethyl)amino]methyl}-1,3-thiazol-4-yl)quinazolin-4-amine dihydrochloride 1173023-85-2 GW 583340 dihydrochloride is an effective inhibitor of dual EGFR/ErbB2 tyrosine kinase with IC50 values of 0.01 and 0.014 μM respectively.
CSN22156 Epertinib 908305-13-5 Epertinib is a potent, oral, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively; Epertinib shows potent antitumor activity.
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.
CSN18252 CP-724714 383432-38-0 CP-724714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, > 640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc.
CSN12702 (E/Z)-CP-724714 537705-08-1 CP-724714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, > 640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc in cell-free assays.
CSN10535 Canertinib dihydrochloride 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.
CSN15701 BMS-690514 859853-30-8 BMS-690514 is a potent and selective inhibitor of epidermal growth factor receptor (EGFR), HER2, and HER4, as well as the VEGF receptor kinases.
CSN18515 BMS-599626 Hydrochloride 873837-23-1 BMS-599626 is an inhibitor of HER1 (IC50 = 20 nM) and HER2 (IC50 = 30 nM).
CSN15811 Sapitinib 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 Allitinib tosylate 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 T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases.
CSN16578 Allitinib 897383-62-9 AST-1306 is an 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.
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 L858R/T790M and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM respectively.
CSN12809 BMS-599626 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.
CSN27781 TAS0728 2088323-16-2
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