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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 | (+)-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. |
| CSN28533 | (2S,4R)-1-((S)-2-(tert-Butyl)-14-(4-(4-((3-chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)quinazolin-6-yl)phenoxy)-4-oxo-6,9,12-trioxa-3-azatetradecan-1-oyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide | 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 | 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 = 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 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. |
| CSN25718 | N-{3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl}-6-(2-{[(2-methanesulfonylethyl)amino]methyl}-1,3-thiazol-4-yl)quinazolin-4-amine 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 | 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. |
| 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 | N-(3-Chloro-4-fluorophenyl)-6-(4-((diethylamino)methyl)piperidin-1-yl)pyrimido[5,4-d]pyrimidin-4-amine | 793726-84-8 | BIBU 1361 dihydrochloride is a selective inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase with IC50 of 3 nM. |
| 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 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 | AG490 | 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 | 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 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 | (2S,4R)-1-((S)-2-(2-(2-(2-(4-(4-((3-Chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)quinazolin-6-yl)phenoxy)ethoxy)ethoxy)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide | 2230821-38-0 | Potent EGFR PROTAC®; also degrades HER2 |
| CSN51376 | Dosimertinib | 2403760-70-1 | |
| CSN51530 | 9-Isopropyl-N2-(4-(4-methylpiperazin-1-yl)phenyl)-N8-(pyridin-3-yl)-9H-purine-2,8-diamine | 1350544-93-2 |
