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EGFR
货号 | 产品名 | CAS号 | 信息 |
---|---|---|---|
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 | WZ-3146 | 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). |
CSN20619 | Tyrphostin RG 14620 | 136831-49-7 | Tyrphostin RG14620 is an EGFR inhibitor of tyrphostin family, which selectively reverses ABCG2-mediated multidrug resistance in cancer cell lines. |
CSN21355 | Tyrphostin AG 528 | 133550-49-9 | Tyrphostin is a potent inhibitor of EGFR protein tyrosine kinase. |
CSN20011 | Theliatinib | 1353644-70-8 | Theliatinib, is a small molecule, epidermal growth factor receptor tyrosine kinase inhibitor with potential antineoplastic and anti-angiogenesis activities. |
CSN20156 | Pyrotinib dimaleate | 1397922-61-0 | Pyrotinib maleate is an irreversible pan-ErbB receptor tyrosine kinase inhibitor, in patients with HER2-Positive metastatic breast cancer. |
CSN19258 | Mavelertinib | 1776112-90-3 | PF-06747775 provides potent EGFR activity against the four common mutants (exon 19 deletion (Del), L858R, and double mutants T790M/L858R and T790M/Del), selectivity over wild-type EGFR, and desirable ADME properties. |
CSN22485 | PF-06459988 | 1428774-45-1 | PF-06459988 is an irreversible inhibitor of T790M-Containing EGFR Mutants. |
CSN23039 | PF-6274484 | 1035638-91-5 | PF 6274484 is a high affinity and potent covalent EGFR kinase inhibitor with Ki of 0.14 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. |
CSN19270 | AZD9291 Dimesylate | N/A | Osimertinib Dimesylate 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 | N1-(2-(Dimethylamino)ethyl)-5-methoxy-N1-methyl-N4-(4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)benzene-1,2,4-triamine | 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. |
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. |
CSN19011 | Naquotinib mesylate | 1448237-05-5 | Naquotinib mesylate is a mutant-selective irreversible EGFR inhibitor with IC50 of 70 nM for NCI-H1650 cell growth,inhibits growth of non-small cell lung cancer (NSCLC) cells with EGFR activating and T790M resistance mutations. |
CSN19010 | Naquotinib | 1448232-80-1 | Naquotinib is an irreversible mutant EGFR inhibitor with potential antineoplastic activity. |
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). |
CSN21195 | Lazertinib | 1903008-80-9 | Lazertinib is a selective inhibitor of mutant EGFR with lowest activity against EGFR wild type. |
CSN18360 | N-(3-Ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine | 610798-31-7 | Icotinib is an EGFR inhibitor with IC50 of 5 nM. EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R) are also its targets. |
CSN18651 | 5,7-Dihydroxy-3-(4-hydroxyphenyl)-4H-chromen-4-one | 446-72-0 | Genistein has multiple biological functions. It can inhibit several tyrosine kinases (IC50 of 0.6 μM for EGFR), inhibits DNA topoisomerase-II and activation of PPARs. Genistein is a phytoestrogen which has selective estrogen receptor modulator properties. |
CSN18050 | Gefitinib HCl | 184475-55-6 | Gefitinib HCl is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. |
CSN18153 | Erlotinib mesylate | 248594-19-6 | Erlotinib mesylate is a directly acting inhibitor of human EGFR tyrosine kinase with an IC50 of 2 nM. |
CSN16725 | N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine hydrochloride | 183319-69-9 | Erlotinib HCl is a directly acting inhibitor of human EGFR tyrosine kinase with an IC50 of 2 nM. |
CSN22392 | EGFR-IN-2 | 1643497-70-4 | EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor. |
CSN19009 | Nazartinib S-enantiomer | 1508256-20-9 | EGF816 S-Enantiomer is the S-enantiomer of EGF816. |
CSN17903 | Nazartinib mesylate | 1508250-72-3 | EGF816 mesylate is a covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min−1 on EGFR(L858R/790M) mutant, respectively. |
CSN16199 | Nazartinib | 1508250-71-2 | EGF816 inhibits mutant EGFR (L858R/790M) with Ki of 31 nM irreversibly and selectively. |
CSN18738 | 2-(5-Fluoro-2-hydroxyphenyl)-2-(1-oxoisoindolin-2-yl)-N-(thiazol-2-yl)acetamide | 1942114-09-1 | EAI045, an allosteric inhibitor, selectively targets drug-resistant EGFR mutants like EGFR-L858R, EGFR-T790M and EGFR-L858R/T790M with IC50 of 0.019 μM, 0.19 μM and 0.002 μM respectively. |
CSN19954 | Cyasterone | 17086-76-9 | Cyasterone is an inhibitor of EGFR that maybe a promising anti-cancer agent espcially in skin carcinoma. |
CSN17871 | Rociletinib HBr | 1446700-26-0 | CO-1686 hydrobromide is an irreversible and orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M (IC50=21 nM). |
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. |
CSN18858 | CHMFL-EGFR-202 | 2089381-40-6 | CHMFL-EGFR-202 can form a covalent bond with Cys797 in a distinct "DFG-in-C-Helix-out" inactive EGFR conformation. |
CSN25283 | CGP52411 | 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. |
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. |
CSN18515 | BMS-599626 HCl | 873837-23-1 | BMS-599626 is an inhibitor of HER1 (IC50 = 20 nM) and HER2 (IC50 = 30 nM). |
CSN16872 | (R)-4-((3-Chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl 2,4-dimethylpiperazine-1-carboxylate | 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). |
CSN20594 | Avitinib | 1557267-42-1 | Avitinib selectively inhibits EGFR L858R/T790M mutant with IC50 of 7.68 nM. It used as antineoplastic drug candidate. |
CSN20602 | N-(3-((2-((3-Fluoro-4-(4-methylpiperazin-1-yl)phenyl)amino)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy)phenyl)acrylamide 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. |
CSN16123 | N-(4-((3-Chloro-4-fluorophenyl)amino)-7-(3-methyl-3-(4-methylpiperazin-1-yl)but-1-yn-1-yl)quinazolin-6-yl)acrylamide | 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 | 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. |
CSN24797 | N-(2-((2-(Dimethylamino)ethyl)(methyl)amino)-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)-6-(2,2,2-trifluoroethoxy)pyridin-3-yl)acrylamide methanesulfonate | 2130958-55-1 | AST2818 mesylate is an EGFR inhibitor. |
CSN21203 | 1-(((4-((4-Fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinolin-7-yl)oxy)methyl)cyclopropanamine dihydrochloride | 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. |
CSN17439 | Anlotinib | 1058156-90-3 | Anlotinib is an EGFR inhibitor which can be used to treat non-small cell lung cancer. |
CSN24709 | AG1557 | 189290-58-2 | AG1557 is a specific EGFR tyrosine kinase inhibitor with pIC50 value of 8.194. |
CSN21119 | 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. |
CSN23735 | (E)-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. |
CSN21882 | AG 555 | 133550-34-2 | AG 555 is an inhibitor of epidermal growth factor receptor (EGFR) with IC50 of 0.7 μM. |
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. |