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EGFR

EGFR

Cat. No. Product Name CAS No. Information
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 (+)-Tyrphostin B44 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 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.
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.
CSN23025 PD0166285 dihydrochloride 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 036 M
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 2,5-dihydroxycinnamate 63177-57-1 Methyl 2,5-dihydroxycinnamate, the erbstatin analog, is an inhibitor of EGF receptor-associated tyrosine kinases.
CSN25434 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.
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 hydrochloride 2134096-03-8 HS-10296 is the third-generation EGFR TKIs which exhibited inhibitory effect on both EGFR-activating mutations and T790M-resistant mutation.
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).
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 Daphnetin 486-35-1 Daphnetin is an inhibitor of EGFR, PKA and PKC with IC50 of 7.67 M, 9.33 M and 25.01 M 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.
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
CSN25556 BI-4020 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 T790ML858R, 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 05 nM and 3 nM also effective in mutation EGFR T790ML858R more potent to ErbB2-overexpressing cells 3000-fold selective for ErbB family than other kinases
CSN13724 AG490   133550-30-8 AG-490 is a broad-spectrum inhibitor that has several targets including EGFR (IC50 2 M), ErbB2 (IC50 13.5 M), STAT3 and JAK2.
CSN25386 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).
CSN24707 (E)-AG 556 133550-41-1 AG 556 is an EGFR kinase inhibitor with IC50 value of 1.1μM, selective over ErbB2 (IC50 > 500 μM).
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 L858RT790M and HER2 with IC50 of 05 nM 04 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
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