||Lapatinib(GW-572016) is an effective ErbB2 and EGFR inhibitor with IC50 of 9.2 and 10.8 nM, respectively.
||Lapatinib ditosylate monohydrate
||Lapatinib is a tyrosine kinase receptor inhibitor used in the therapy of advanced breast cancer and other solid tumors. Lapatinib therapy is associated with transient elevations in serum aminotransferase levels and rare instances of clinically apparent acute liver injury.
||Sanguinarine chloride, a benzophenanthridine alkaloid, stimulates apoptosis by activating the production of reactive oxygen species (ROS).
||Erlotinib (NSC 718781; OSI-744; R1415) is an EGFR inhibitor (IC50 of 2 nM). It is >1000-fold more sensitive for EGFR than human v-Abl or c-Src.
||Erlotinib is a direct acting inhibitor against human EGFR tyrosine kinase (IC50: 2 nM). Erlotinib hydrochloride (trade name Tarceva) is a drug used in the treatment of pancreatic Y, non-small cell lung Y and some other types of Y.
||Lidocaine Hydrochloride hydrate
||Lidocaine Hydrochloride hydrate is an amide local anesthetic, has anti-inflammatory property.
||Vandetanib is a Kinase Inhibitor.
||Genistein is an isoflavonoid derived from soy products. It inhibits protein-tyrosine kinase and topoisomerase-II (DNA TOPOISOMERASES, TYPE II), with antineoplastic and antitumor activities.
||PD153035 hydrochloride (ZM 252868; AG 1517) is a effective and selective inhibitor of EGFR (Ki: 5.2 pM, IC50: 29 pM); few influence against FGFR, PGDFR, InsR, CSF-1, and Src.
||Afatinib (BIBW2992) Dimaleate
||Afatinib is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.
||WHI-P154 is a potent JAK3 inhibitor.
||ZZZM 323881 hydrochloride is a potent and selective VEGFR2 inhibitor.
||WHI-P180 is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 uM, respectively.
||WHI-P258 is a dimethoxyquinazoline inhibitor of JAK3. This compound binds JAK3 weakly and may be used as a JAK-binding negative control in the development of new therapeutics.
||PD153035 hydrochloride is an effective and selective inhibitor of EGFR (Ki/IC50: 5.2/29 pM, in cell-free assays); little inhibitory against FGFR, PGDFR, InsR, CSF-1 and Src.
||AG-1478 (Tyrphostin AG-1478) is a selective EGFR inhibitor.
||WS3, a β cell proliferation inducer, regulates Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.
||AG-18 inhibits EGFR with IC50 of 35 μM.
||WS6, a β cell proliferation inducer, regulates Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.
||AEE788 has been used in trials studying the treatment of Cancer, Glioblastoma Multiforme, and Brain and Central Nervous System Tumors.
||CL-387785(EKI785; WAY-EKI 785) is an irreversible inhibitor of EGFR（IC50： 370+/-120 pM）; is able to overcome resistance caused by the T790M mutation on a functional level.
||Endoxifen (EDX) is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptors that also inhibits aromatase activity.
||Afatinib is a tyrosine kinase receptor inhibitor that is used in the therapy of selected forms of metastatic non-small cell lung cancer.
||Icotinib Hydrochloride is the hydrochloride salt form of icotinib, an orally available quinazoline-based inhibitor of EGFR, with potential antineoplastic activity. Icotinib selectively inhibits the wild-type and several mutated forms of EGFR tyrosine kinase. This may lead to an inhibition of EGFR-me
||Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor (IC50: 59/92 nM) for HER2 and EGFR, respectively. Neratinib binds to the HER-2 receptor irreversibly, thereby reducing autophosphorylation in cells, apparently by targeting a cysteine residue in the ATP-binding pocke
||Pelitinib (EKB-569) is an effective irreversible EGFR inhibitor (IC50: 38.5 nM).
||Irbinitinib(ARRY-380; ONT-380) is a potent and selective HER2 inhibitor (IC50: 8 nM).
||Rociletinib is an orally available small molecule, irreversible inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity.
||KI8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM.
||ZM 39923 hydrochloride
||ZM 39923 hydrochloride is a JAK1/3 inhibitor with pIC50 of 4.4/7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to be sensitive to transglutaminase.
||Tyrphostin 9 is an Agricultural acaricide, now superseded. Tyrphostin 9 is firstly designed as an EGFR inhibitor
||Dacomitinib (PF299804, PF299)
||Dacomitinib(PF299804; PF-00299804) is a highly selective, orally bioavailable small-molecule inhibitor of the HER family of tyrosine kinases with IC50 of 6, 45.7 and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.
||Osimertinib is a small molecule tyrosine kinase receptor inhibitor and antineoplastic agent that is used in the therapy of selected forms of advanced non-small cell lung cancer (NSCLC).
||AZ5104 is a potent EGFR inhibitor.
||Canertinib dihydrochloride is the hydrochloride salt of an orally bio-available quinazoline with potential antineoplastic and radiosensitizing activities.
||ARRY-380 is a potent and selective HER2 inhibitor.
||AG-490 (Tyrphostin AG 490) is an inhibitor of EGFR (IC50: 0.1 μM). It is 135-fold more selective for EGFR than ErbB2, also inhibits JAK2 with no effect to Lyn, Lck, Syk, Btk, and Src.
||PD173074 is an effective FGFR1 inhibitor (IC50: 25 nM) and also inhibits VEGFR2 (IC50: 100-200 nM) in cell-free assays. The selectivity is higher ~1000-fold for FGFR1 than PDGFR and c-Src.
||Mutant EGFR inhibitor
||Mutant EGFR inhibitor is a selective and potent Mutated EGFR inhibitor, inhibits L858R activating mutant, the Exonl9 deletion activating mutant and the T790M resistance mutant.
||Daphnetin, a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.
||Biochanin A is an isoflavone derivative isolated from red clover Trifolium pratense with anticarcinogenic properties. Biochanin A is a naturally occurring fatty acid amide hydrolase (FAAH) inhibitor.
||Ginsenoside Rh2, an extract of red Panax ginseng, is a potent anti-inflammatory and anticancer drug.
||Chrysophanic acid is an EGFR/mTOR pathway inhibitor, which can be found in rhubarb, and sorrel.
||Avitinib, also known as AC0010 or AC0010MA, is an orally available, irreversible, epidermal growth factor receptor (EGFR) mutant-selective inhibitor, with potential antineoplastic activity. Upon oral administration, avitinib covalently binds to and inhibits the activity of mutant forms of EGFR, incl
||Brigatinib is a excellently effective and specific ALK inhibitor( IC50 =0.6 nM).
||CUDC-101 is a potent inhibitor of HDAC, EGFR and HER2 with IC50s of 4.4, 2.4 and 15.7 nM, respectively.
||NS1643 is a potent human ether-a-go-go related gene (hERG) KV11.1 channel activator with EC50 of 10.5 μM.
||Ginsenoside Rg3 possess an ability to inhibit the lung metastasis of tumor cells via inhibition of the adhesion and invasion of tumor cells. It inhibits the proliferation of human umbilical vein endothelial cells(HUVEC) and has anti-angiogenesis activities.
||Nazartinib (EGF816, NVS-816) is a covalent, irreversible, mutant-selective EGFR inhibitor that has nanomolar inhibitory potency against activating mt (L858R, ex19del) and T790M mt, with up to 60-fold selectivity over wild type (wt) EGFR in vitro.
||RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor (IC50: 4 μM).
||EBE-A22 is a derivative of PD 153035 which can inhibit ErbB-1-phosphorylation, whereas EBE-A22 is inactive.
||Brigatinib is a highly potent and selective ALK inhibitor.
||AZD-9291 mesylate is an irreversible and mutant-selective EGFR inhibitor.
||AZD3759 is an orally active, effective and central nervous system-penetrant EGFR inhibitor. The IC50 values were 0.2, 0.3 and 0.2 nM for EGFR L858R mutant, TK wild-type, and Exon 19Del enzymes, respectively.
||Avitinib maleate is a pyrrolopyrimidine-based irreversible epidermal growth factor receptor (EGFR) inhibitor.
||Cyasterone, a natural EGFR inhibitor, can inhibit the growth of A549 and MGC823 cells, via regulating EGFR signaling pathway, it may be a promising anti-cancer agent. Cyasterone has antifeeding activity.
||CP-724714 is an effective and selective HER2/ErbB2 inhibitor (IC50: 10 nM), >640-fold selectivity against EGFR, Abl, InsR, PDGFR, IRG-1R, Src, VEGFR2, c-Met etc.
||lavendustin A is a potent, cell-permeable inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase.
||AG-494 is an inhibitor of epidermal growth factor receptor kinase.
||AZD3759 (hydrochloride) is an effective, orally active and central nervous system-penetrant?EGFR?inhibitor. At Km?ATP concentrations, the?IC50s are 0.2/0.3/0.2 nM for EGFR (L858R)/EGFR (wt)/EGFR (exon 19Del).
||MTX-211, an inhibitor of EGFR and PI3K, is used for the therapy of cancer and other diseases.
||Tyrphostin AG 555
||AG 555 is an EGFR tyrosine kinase inhibitor.
||CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR.
||Brivanib is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β. Phase 3.
||TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. Phase 1.
||CP-724,714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, >640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc. Phase 2.
||Saracatinib (AZD0530) is an effective Src inhibitor (IC50: 2.7 nM), and effective to c-Yes, Lyn, Fyn, Fgr, Blk and Lck; less active for Abl and EGFR (L858R and L861Q).
||AZD8931, a reversible, ATP competitive inhibitor of EGFR(IC50=4 nM), ErbB2(IC50=3 nM) and ErbB3(IC50=4 nM), is more effective over Gefitinib or Lapatinib against NSCLC cell, 100-fold more specific for the ErbB family over MNK1 and Flt.
||Mubritinib (TAK 165)
||Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM.
||Canertinib is a pan-erbB tyrosine kinase inhibitor which work against esophageal squamous cell carcinoma in vitro and in vivo. Canertinib treatment significantly affects tumour metabolism, proliferation and hypoxia as determined by PET.
||Icotinib is an orally available quinazoline-based inhibitor of epidermal growth factor receptor (EGFR), with potential antineoplastic activity.
||PP1, a specific and effective Src inhibitor, is with IC50 for Lck/Fyn is 5 nM/ 6 nM, respectively.
||Benidipine HCl, a hydrochloride salt form of benidipine, is used as a blocker of dihydropyridine calcium channel.
||Lapatinib (GW-572016) Ditosylate
||Lapatinib Ditosylate, an effective EGFR and ErbB2 inhibitor, is with IC50 of 10.8 and 9.2 nM for EGFR and ErbB2, respectively.
||WZ4002 is a mutant-selective EGFR inhibitor for EGFR(L858R) and EGFR(T790M) with IC50 of 2 nM/8 nM.
||PP2 is a effective inhibitor of Lck/Fyn (IC50:4/5 nM) , ~100-fold less potent to EGFR, inactive for ZAP-70, PKA and JAK2.
||OSI-420 is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM).
||AST-1306 is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, respectively.
||Butein, a plant polyphenol, is isolated from Rhus verniciflua. It can inhibit the activation of protein tyrosine kinase, NF-κB and STAT3, and also can inhibit EGFR.
||OSI-420 (Desmethyl Erlotinib,CP-473420) is an active metabolite of erlotinib which is an orally active EGFR tyrosin kinase inhibitor with IC50 of 2 and 20 nM for? human EGFR and EGFR autophosphorylation in tumor cells.
||Tyrphostin AG 879
||Tyrphostin AG 879 effectively inhibits HER2/ErbB2 (IC50: 1 μM), 100- and 500-fold higher selective to ErbB2 than EGFR and PDGFR.
||WZ3146 is a mutant-selective irreversible inhibitor of EGFR(L858R) and EGFR(E746_A750) with IC50 of 2 nM and 2 nM; does not inhibit ERBB2 phosphorylation (T798I).
||WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).
||EAI045， an allosteric inhibitor， targets towards drug-resistant EGFR mutants but avoids the wild-type receptor.
||Olmutinib (HM61713, BI 1482694)
||Olmutinib is an orally available small molecule, a mutant-selective inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Olmutinib binds to and inhibits mutant forms of EGFR, thereby leading to cell death of EGFR-expressing tumor cells. As this agent is select
||PD168393 is an irreversible EGFR inhibitor (IC50: 0.70 nM), irreversibly alkylate Cys-773; inactive against PKC, FGFR, PDGFR, and insulin.
||Lavendustin C is a potent inhibitor of epidermal growth factor (EGF) receptor-associated tyrosine kinase.