HER2
| 货号 | 产品名 | CAS号 | 信息 |
|---|---|---|---|
| FB04409 | XL647 | 781613-23-8 | XL647 or tesevatinib inhibits EGFR, HER2, VEGFR and EphB4 with potential antineoplastic activity. |
| FB08916 | 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. |
| FB00749 | 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. |
| FB17212 | 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. |
| FB00811 | 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. |
| FB00601 | Poziotinib | 1092364-38-9 | Poziotinib is an irreversible Pan-HER inhibitor with IC50s of 3/5/23 nM for HER1/HER2/HER4 respectively. |
| FB09889 | 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. |
| FB05357 | 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. |
| FB06534 | 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. |
| FB17734 | 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. |
| FB03337 | Lapatinib Ditosylate | 388082-77-7 | Lapatinib ditosylate is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM, respectively. |
| FB06973 | 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. |
| FB17165 | GW 583340 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. |
| FB11778 | 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. |
| FB01649 | 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. |
| FB04934 | 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. |
| FB02561 | CP-724714 (Random Configuration) | 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. |
| FB09165 | 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. |
| FB07143 | 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. |
| FB06886 | BMS-599626 HCl | 873837-23-1 | BMS-599626 is an inhibitor of HER1 (IC50 = 20 nM) and HER2 (IC50 = 30 nM). |
| FB08315 | 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. |
| FB09964 | 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 T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases. |
| FB07150 | AST-1306 | 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. |
| FB01119 | 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. |
| FB10660 | 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. |
| FB06437 | 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. |