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EGFR

EGFR

货号 产品名 CAS号 信息
CSN15826 ZM 306416 690206-97-4 ZM-306416 is an inhibitor of VEGFR (Flk-1 or KDR) and Flt with IC50 of 100 nM and 2 μM. It also shows inhibition activity against Src and Abl with IC50 values of 0.33μM and 1.3μM, respectively.
CSN23885 ZD-4190 413599-62-9 ZD-4190 is an inhibitor of vascular endothelial cell growth factor receptor 2 (VEGFR2) and epidermal growth factor receptor (EGFR) signalling.
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.
CSN25719 AG 835 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.
CSN26110 EGFR-IN-7 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.
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 Isopropyl 2-((5-acrylamido-4-((2-(dimethylamino)ethyl)(methyl)amino)-2-methoxyphenyl)amino)-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate 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.
CSN28533 SJF 1521 2230821-40-4 Selective EGFR PROTAC.
CSN20157 Pyrotinib 1269662-73-8 Pyrotinib is an irreversible pan-ErbB receptor tyrosine kinase inhibitor, in patients with HER2-Positive metastatic breast cancer.
CSN16204 1-(4-((4-((3,4-Dichloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)piperidin-1-yl)prop-2-en-1-one 1092364-38-9 Poziotinib is an irreversible Pan-HER inhibitor with IC50s of 3/5/23 nM for HER1/HER2/HER4 respectively.
CSN23025 PD0166285 2HCl 212391-63-4 PD 166285 inhibited Src nonreceptor tyrosine kinase, fibroblast growth factor receptor-1, epidermal growth factor receptor and platelet-derived growth factor receptor beta subunit (PDGFR-beta), tyrosine kinases with half-maximal inhibitory potencies (IC50 values) of 8.4 +/- 2.3 nM (n = 6), 39.3 +/- 2.8 nM (n = 16), 87.5 +/- 13.7 nM (n = 6) and 98.3 +/- 7.9 nM (n = 16), respectively.
CSN22616 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).
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.
CSN26226 MTX-211 1952236-05-3 MTX-211 is a dual inhibitor of EGFR and PI3K, used for the treatment of cancer and other diseases.
CSN28508 MS154 2550393-21-8 MS 154 is a potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant epidermal growth factor receptor (EGFR), comprising a cereblon-binding moiety joined by a linker to gefitinib. MS 154 decreases EGFR protein levels, inhibits downstream signaling in and inhibits proliferation of mutant EGFR-bearing lung cancer cells (DC50 values are 11 and 25 nM in HCC-827 and H3255 cells, respectively; Dmax > 95% at 50 nM), but not in WT-EGFR-bearing ovarian and lung cancer cells lines. It is bioavailable in mice following ip administration.
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.
CSN25720 Methyl 3-(2,5-dihydroxyphenyl)acrylate 63177-57-1 Methyl 2,5-dihydroxycinnamate, the erbstatin analog, is an inhibitor of EGF receptor-associated tyrosine kinases.
CSN25434 4,9-Dimethoxy-7-methyl-5H-furo[3,2-g]chromen-5-one 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.
CSN24696 JND3229 2260886-64-2 JND3229 is a new highly potent EGFR(C797S) inhibitor with IC50 values of 5.8nM, 30.5nM and 6.8nM for EGFR (L858R/T790M/C797S), EGFR (T790M, L858R) and EGFR, respectively.
CSN26106 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.
CSN26639 JBJ-04-125-02 2060610-53-7 JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFRL858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFRL858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities[1].
CSN26167 (Rac)-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.
CSN24731 Cyanidin-3-O-galactoside chloride 27661-36-5 Idaein chloride is a glycoside derivative of cyanidin, a potent inhibitor of EGFR, used in comparative analysis of anti-EGF activity in cancer cells.
CSN25621 Almonertinib 1899921-05-1 HS-10296 is the third-generation EGFR TKIs which exhibited inhibitory effect on both EGFR-activating mutations and T790M-resistant mutation.
CSN25641 Almonertinib 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.
CSN25718 GW583340 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.
CSN22297 Gefitinib-based PROTAC 3 2230821-27-7 Gefitinib-based PROTAC 3 is a VHL-recruiting PROTAC that induces the degradation of EGFR and EGFR mutants with DC50 of 11.7 nM and 22.3 nM for HCC827 cell (Exon 19 del) and H3255 cell (L858R).
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.
CSN26637 EMI48 34564-13-1 EMI48, the derivative of EMI1, displays greater potency toward mutant EGFR than EMI1. EMI48 inhibits EGFR triple mutants[1].
CSN26544 EGFR-IN-8 2407957-87-1 EGFR-IN-8 is a dual EGFR and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC[1].
CSN28785 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.
CSN27394 Olafertinib 1660963-42-7 EGFR-IN-3 is an epidermal growth factor receptor (EGFR) inhibitor.
CSN25629 EGFR-IN-12 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.
CSN10745 7,8-Dihydroxy-2H-chromen-2-one 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 (E)-N-(4-((3-Chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)-4-(piperidin-1-yl)but-2-enamide 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.
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.
CSN25721 BIBU1361 793726-84-8 BIBU 1361 dihydrochloride is a selective inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase with IC50 of 3 nM.
CSN25556 (R,E)-11,26,7-Trimethyl-56-((4-methylpiperazin-1-yl)methyl)-52,53-dihydro-11H,51H-11-oxa-4-aza-5(2,1)-benzo[d]imidazola-2(2,4)-pyridina-1(4,5)-pyrazolacycloundecaphan-3-one 2664214-60-0 BI-4020 is a noncovalent, new-generation, wild-type EGFR sparing, macrocyclic tyrosine kinase inhibitor.
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.
CSN13724 (E)-N-Benzyl-2-cyano-3-(3,4-dihydroxyphenyl)acrylamide 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.
CSN25386 N-(3-Chlorophenyl)-6,7-dimethoxyquinazolin-4-amine 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).
CSN12703 (S,E)-N-(4-((3-Chloro-4-fluorophenyl)amino)-7-((tetrahydrofuran-3-yl)oxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide 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.
CSN28532 SJF 1528 2230821-38-0 Potent EGFR PROTAC®; also degrades HER2
CSN52442 (E)-2-Cyano-3-(3,4-dihydroxyphenyl)-N-(4-phenylbutyl)acrylamide 133550-41-1
CSN51376 Dosimertinib-d3 2403760-70-1
CSN51530 Ruserontinib 1350544-93-2
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