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EGFR

EGFR

货号 产品名 CAS号 信息
CSN16336 XL647 781613-23-8 XL647 or tesevatinib inhibits EGFR, HER2, VEGFR and EphB4 with potential antineoplastic activity.
CSN16551 WZ8040 1214265-57-2 WZ8040 is a mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).
CSN16109 WZ4002 1213269-23-8 WZ4002 is an irreversible inhibitor of mutant EGFR (L858R) and EGFR (T790M) with IC50 of 2 nM and 8 nM respectively.
CSN16526 WZ3146 1214265-56-1 WZ3146 is a mutant-selective irreversible inhibitor of EGFR (L858R) and EGFR (E746_A750) with IC50 of 2 nM and 2 nM and does not inhibit ERBB2 phosphorylation (T798I).
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.
CSN16204 Poziotinib 1092364-38-9 Poziotinib is an irreversible Pan-HER inhibitor with IC50s of 3/5/23 nM for HER1/HER2/HER4 respectively.
CSN11666 Pelitinib 257933-82-7 Pelitinib irreversiblly inhibits EGFR with IC50 of 38.5 nM.
CSN16908 PD168393 194423-15-9 PD168393 is an inhibitor that targets EGFR with IC50 of 0.70 nM irreversibly. It is not active against insulin, PDGFR, FGFR and PKC.
CSN13798 PD158780 171179-06-9 PD158780, a pyridopyrimidine derivative, is reversible inhibitor of ErbB receptor family (IC50s for EGFR, ErbB2 and ErbB2/ErbB4 are 0.008 nM, 49 nM and 52 nM respectively).
CSN12357 PD153035 153436-54-5 PD153035 is EGFR inhibitor with Ki and IC50 of 5.2 pM and 29 pM and could rapidly suppress autophosphorylation of EGFR.
CSN12700 PD153035 HCl 183322-45-4 PD153035 hydrochloride is an reversible inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM.
CSN13923 Osimertinib Mesylate 1421373-66-1 Osimertinib Mesylate is a selective inhibitor of mutant EGFR with IC50s of 12 nM and 1 nM for L858R and L858R/T790M in enzyme assay respectively.
CSN13922 Osimertinib   1421373-65-0 Osimertinib 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).
CSN16873 Osimertinib DA 1421372-66-8 Osimertinib DA is a desacryl analogue of Osimertinib, is an intermediate inhibitor of mutated EGFR, including L858R EGFR, Exonl9 deletion and T790M resistance mutant.
CSN15680 OSI-420 183320-51-6 OSI-420 is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM).
CSN17738 Olmutinib 1353550-13-6 Olmutinib inhibits EGFR with IC50 values of 9.2 nM and 10 nM in HCC827 (expressing EGFR-del 19) and H1975 (expressing EGFR-L858R/T790M) cell respectively. It is a new targeted drug for the treatment of mutation-positive NSCLC.
CSN17827 Mutant EGFR Inhibitor 1421373-62-7 Mutant EGFR inhibitor is a selective and potent Mutated EGFR inhibitor (L858R activating mutant, the Exonl9 deletion activating mutant and the T790M resistance mutant).
CSN11268 Lapatinib 231277-92-2 Lapatinib is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM, respectively.
CSN12862 Lapatinib Ditosylate Hydrate 388082-78-8 Lapatinib ditosylate inhibits EGFR and ErbB2 with IC50 of 10.8 nM and 9.2 nM.
CSN12937 Icotinib HCl 1204313-51-8 Icotinib hydrochloride is a potent and specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with an IC(50) of 5 nM, including it's mutants of EGFR (L858R), EGFR (L861Q), EGFR (T790M) and EGFR (T790M, L858R).
CSN11084 Gefitinib   184475-35-2 Gefitinibis an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively, and interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells.
CSN10931 Erlotinib 183321-74-6 Erlotinib is an EGFR inhibitor with IC50 of 2 nM, > 1000-fold more sensitive for EGFR than human c-Src or v-Abl.
CSN16725 Erlotinib HCl 183319-69-9 Erlotinib HCl is a directly acting inhibitor of human EGFR tyrosine kinase with an IC50 of 2 nM.
CSN16199 EGF816 1508250-71-2 EGF816 inhibits mutant EGFR (L858R/790M) with Ki of 31 nM irreversibly and selectively.
CSN10745 Daphnetin 486-35-1 Daphnetin is an inhibitor of EGFR, PKA and PKC with IC50 of 7.67 μM, 9.33 μM and 25.01 μM respectively. It derives from plants of the genus Daphne.
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.
CSN15847 CUDC-101 1012054-59-9 CUDC-101 inhibits HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM and 15.7 nM, respectively.
CSN13912 CO-1686 1374640-70-6 CO-1686 functions as an irreversible and mutant-selective inhibitor of EGFRL858R/T790M and EGFRWT with Ki of 21.5 nM and 303.3 nM respectively.
CSN17167 CNX-2006 1375465-09-0 CNX-2006 is an irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.
CSN16222 CL-387785 194423-06-8 CL-387785 irreversibly inhibits EGFR with IC50 of 370 pM and shows inhibition of the functional effects of mutations T790M.
CSN12261 Canertinib 267243-28-7 Canertinib 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.
CSN10535 Canertinib 2HCl 289499-45-2 Canertinib dihydrochloride, 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.
CSN10516 Butein 487-52-5 Butein, a plant polyphenol isolated from Rhus verniciflua, is able to inhibit the activation of protein tyrosine kinase, NF-κB and STAT3, also inhibits EGFR.
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.
CSN15747 BIBX 1382 196612-93-8 BIBX 1382 is a potent, selective inhibitor of EGFR tyrosine kinase (IC50 = 3 nM) and displays > 1000-fold lower potency against ErbB2 (IC50 = 3.4 μM) and a range of other related tyrosine kinases (IC50 > 10 μM).
CSN16872 AZD3759 1626387-80-1 AZD3759 is an inhibitor of EGFR (WT), EGFR (L858R) and EGFR (exon 19 deletion) (IC50s values are 0.3 nM, 0.2 nM and 0.2 nM, respectively).
CSN15755 AZ5104 1421373-98-9 AZ5104 is an irreversible inhibitor of EGFR-L858R/T790M, EGFR-L858R, EGFR-L861Q, and EGFR (IC50s of < 1 nM, 6 nM, 1 nM, and 25 nM respectively). AZ5104 is the demethylated metabolite of AZD-9291.
CSN16123 AV-412 451492-95-8 AV-412 is an inhibitor of EGFR (IC50 = 0.5-2 nM), ErbB2 (IC50=19 nM), Abl receptor (IC50 = 41nM), mutant EGFR-L858R (IC50=0.51 nM) and EGFR-T790M (IC50=0.79 nM). It also inhibits autophosphorylation of EGFR and ErbB2 with IC50s of 43 nM and 282 nM, respectively.
CSN16948 AV-412 Tosylate 451493-31-5 AV-412 is a potent dual inhibitor of EGFR and ErbB2(IC50=19 nM) tyrosine kinases, including the mutant EGFR(L858R IC50=0.51 nM, T790M IC50=0.79 nM). It inhibits autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM.
CSN16578 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.
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.
CSN13724 AG-490 133550-30-8 AG-490 is a broad-spectrum inhibitor that has several targets including EGFR (IC50 = 2 μM), ErbB2 (IC50 = 13.5 μM), STAT3 and JAK2.
CSN10228 AG 18 118409-57-7 AG-18 is an inhibitor of epidermal growth factor receptor (EGFR) kinase with IC50 of 35 μM.
CSN12358 AG-1478 153436-53-4 AG-1478 selectively inhibits EGFR with IC50 of 3 nM in cell-free assay.
CSN23735 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.
CSN12371 Afatinib mixture 439081-18-2 Afatinib is an irreversible inhibitor of pan-ErbB inhibitor with IC50 values of 0.4nM, 0.5nM, 10nM, 14nM and 1nM for EGFR (L858R), EGFR (wt), EGFR (L858R/T790M), HER2 and ErbB4, respectively.
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.
CSN16035 Afatinib Dimaleate 850140-73-7 Afatinib dimaleate is an irreversible inhibitor of EGFR and HER2, the IC50s for EGFR (wt), EGFR (L858R), EGFR (L858R/T790M) and HER2 are 0.5 nM, 0.4 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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