EGFR
| 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. |
| FB00752 | Tyrphostin RG14620 | 136831-49-7 | Tyrphostin RG14620 is an EGFR inhibitor of tyrphostin family, which selectively reverses ABCG2-mediated multidrug resistance in cancer cell lines. |
| FB10084 | AG 528 | 133550-49-9 | Tyrphostin is a potent inhibitor of EGFR protein tyrosine kinase. |
| FB17164 | Tyrphostin B44, (+) enantiomer | 133550-37-5 | Tyrphostin B44, (+) enantiomer is an inhibitor of EGFR with IC50 of 0.86 μM. It is slightly less active than the (-) enantiomer. |
| FB17194 | TQB3804 | 2267329-76-8 | TQB3804 is the forth-generation EGFR inhibitor with IC50 values of 7.92nM,0.218nM and 0.16nM for EGFR(WT), EGFR (C797S/T790M/del19) and EGFR (L858R/T790M/C797S), respectively. |
| FB10893 | Theliatinib | 1353644-70-8 | Theliatinib, is a small molecule, epidermal growth factor receptor tyrosine kinase inhibitor with potential antineoplastic and anti-angiogenesis activities. |
| 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. |
| FB11063 | Pyrotinib Maleate | 1397922-61-0 | Pyrotinib maleate is an irreversible pan-ErbB receptor tyrosine kinase inhibitor, in patients with HER2-Positive metastatic breast cancer. |
| FB11064 | Pyrotinib | 1269662-73-8 | Pyrotinib is an irreversible pan-ErbB receptor tyrosine kinase inhibitor, in patients with HER2-Positive metastatic breast cancer. |
| FB00601 | Poziotinib | 1092364-38-9 | Poziotinib is an irreversible Pan-HER inhibitor with IC50s of 3/5/23 nM for HER1/HER2/HER4 respectively. |
| FB11372 | PF-06459988 | 1428774-45-1 | PF-06459988 is an irreversible inhibitor of T790M-Containing EGFR Mutants. |
| FB12621 | PF 6274484 | 1035638-91-5 | PF 6274484 is a high affinity and potent covalent EGFR kinase inhibitor with Ki of 0.14 nM. |
| FB12150 | NSC-228155 | 113104-25-9 | NSC228155 can enhance the tyrosine phosphorylation of EGFR via binding to the dimerization domain II. It blocks KIX-KID interaction as well (IC50 = 0.36 μM). |
| 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. |
| 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. |
| FB17171 | Methyl 2,5-dihydroxycinnamate | 63177-57-1 | Methyl 2,5-dihydroxycinnamate, the erbstatin analog, is an inhibitor of EGF receptor-associated tyrosine kinases. |
| FB11593 | Lazertinib | 1903008-80-9 | Lazertinib is a selective inhibitor of mutant EGFR with lowest activity against EGFR wild type. |
| FB12511 | Lavendustin A | 125697-92-9 | Lavendustin A is a potent, cell-permeable inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase with IC50 of 11 nM. |
| FB16636 | Khellin | 82-02-0 | Khellin, a naturally occurring furochromone, is an EGFR inhibitor with an IC50 of 0.15 µM. Khelline has anti-proliferative activity in vitro. Khellin has antispasmodic and coronary vasodilator effects. |
| FB17198 | JCN037 | 2305154-31-6 | JCN037 is a potent EGFR inhibitor with IC50 values of 2.49 nM, 3.95 nM and 4.48 nM for EGFR, p-wtEGFR and pEGFRvⅢ, respectively. It displayed potent activity against EGFR amplified/mutant patient-derived cell cultures, significant BBB penetration (2:1 brain-to-plasma ratio), and superior efficacy in an EGFR-driven orthotopic glioblastoma xenograft model. |
| FB17250 | JBJ-04-125-02 | 2140807-05-0 | JBJ-04-125-02 is a mutant-selective EGFR allosteric inhibitor with IC50 of 0.26 nM for EGFRL858R/T790M. As a single agent, it can inhibit cell proliferation and EGFRL858R/T790M/C797S signaling in vitro and in vivo. |
| FB16832 | HS-10296 | 1899921-05-1 | HS-10296 is the third-generation EGFR TKIs which exhibited inhibitory effect on both EGFR-activating mutations and T790M-resistant mutation. |
| FB16852 | HS-10296 HCl | 2134096-03-8 | HS-10296 is the third-generation EGFR TKIs which exhibited inhibitory effect on both EGFR-activating mutations and T790M-resistant mutation. |
| 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. |
| FB19903 | EGFR-IN-5 | 2225887-26-1 | EGFR-IN-5 is an inhibitor of EGFR with IC50 values of 10.4 nM, 1.1 nM, 34 nM and 7.2 nM for EGFR, EGFRL858R, EGFRL858R/T790M, and EGFRL858R/T790M/C797S, respectively. It could suppress EGFR phosphorylation in a dose-dependent manner in HCC827 cell line and significantly induce the apoptosis of HCC827 cells. |
| FB17987 | EGFR-IN-3 | 1660963-42-7 | EGFR-IN-3 is an epidermal growth factor receptor (EGFR) inhibitor. |
| FB11997 | EGFR-IN-2 | 1643497-70-4 | EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor. |
| FB16830 | EGFR Inhibitor | 879127-07-8 | EGFR Inhibitor is a potent, ATP-competitive and highly selective EGFR inhibitor with IC50 values of 21nM, 63nM and 4nM for EGFR, EGFR (L858R) and EGFR (L861Q), respectively. It blocked EGF-induced EGFR autophosphorylation in U-2OS cells at 10µM. |
| 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. |
| FB16489 | CGP 52411 | 145915-58-8 | CGP 52411 inhibited the EGF-R protein-tyrosine kinase in vitro with high selectivity. In cells, CGP52411 selectively inhibited both ligand-induced EGF-R and p185c-erbB2 autophosphorylation and c-fos mRNA induction. |
| 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). |
| FB17176 | BIBU 1361 dihydrochloride | 793726-84-8 | BIBU 1361 dihydrochloride is a selective inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase with IC50 of 3 nM. |
| FB16762 | BI-4020 | N/A | BI-4020 is a noncovalent, new-generation, wild-type EGFR sparing, macrocyclic tyrosine kinase inhibitor. |
| FB07196 | Avitinib | 1557267-42-1 | Avitinib selectively inhibits EGFR L858R/T790M mutant with IC50 of 7.68 nM. It used as antineoplastic drug candidate. |
| FB07197 | Avitinib Maleate | 1557268-88-8 | Avitinib maleate, the maleate salt form of avitinib, selectively inhibits EGFR L858R/T790M mutant with IC50 of 7.68 nM. It used as antineoplastic drug candidate. |
| FB16053 | AST2818 mesylate | 2130958-55-1 | AST2818 mesylate is an EGFR inhibitor. |
| 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. |
| FB11600 | Anlotinib 2HCl | 1360460-82-7 | Anlotinib is an inhibitor of receptor tyrosine kinase (RTK), including vascular endothelial growth factor receptor type 2 (VEGFR2) and type 3 (VEGFR3), and shows antineoplastic and anti-angiogenic activities. |
| FB00751 | AG-494 | 133550-35-3 | AG-494 is an inhibitor of EGFR with an IC50 value of 0.7 µM and it is inactive toward ErbB2, PDGFR and insulin receptor kinase. |
| FB16606 | AG 1478 hydrochloride | 170449-18-0 | AG-1478 hydrochloride (Tyrphostin AG-1478 hydrochloride) is a selective EGFR tyrosine kinase inhibitor with IC50 of 3 nM. AG-1478 hydrochloride has antiviral effects against HCV and encephalomyocarditis virus (EMCV). |
| FB15240 | AG 99 | 122520-85-8 | AG 99 is an EGF receptor kinase inhibitor with IC50 of 10 µM in the human epidermoid carcinoma cell line A431. |
| FB00750 | AG 555 | 133550-34-2 | AG 555 is an inhibitor of epidermal growth factor receptor (EGFR) with IC50 of 0.7 μM. |
| 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. |
| FB15903 | AG-1557 | 189290-58-2 |