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Catalog No.
Product Name
Application
Product Information
Citations
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ALK/EGFR inhibitor
HG-14-10-04 is a potent and specific ALK inhibitor with IC50 of 20 nM. -
Her3 (ErbB3) ligand
TX1-85-1 is ErbB3 inhibitor. TX2-121-1 may exert Her3-dependent pharmacology through an allosteric mechanismthereby disrupting interactions between Her3 and other proteins such as Her3 or cMet consistent with results presented here and distinct from conventional kinase inhibitors, which block catalytic function. -
HER2 inhibitor
ARRY-380 is an orally bioavailable inhibitor of the human epidermal growth factor receptor tyrosine kinase ErbB-2 (also called HER2) with potential antineoplastic activity. -
irreversible EGFR inhibitor
Avitinib (AC0010) is a pyrrolopyrimidine-based irreversible EGFR inhibitor that is mutation-selective with IC50 value of 0.18 nM against EGFR L858R/T790M double mutations, nearly 43-fold greater potency over wild-type EGFR (IC50 value, 7.68 nM). It has comparable anti-tumor activity and tolerated toxicity. -
EGFR inhibitor
Lazertinib (YH25448,GNS-1480) is a potent, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R and Wild type EGFR respectively, showing much higher IC50 values aganist ErbB2 and ErbB4. -
EGFR inhibitor
Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant. -
T790M-Containing EGFR Mutants inhibitor
PF-06459988 is an irreversible inhibitor of T790M-Containing EGFR Mutants. -
EGFR inhibitor
Naquotinib mesylate (ASP8273 mesylate) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR. -
EGFR/HER2 inhibitor
Tarloxotinib bromide (TH-4000) is an irreversible EGFR/HER2 inhibitor. -
Raf/EGFR inhibitor
Lifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively. -
EGFR inhibitor
Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFRL858R, EGFRExon 19 deletion and EGFRT790M. -
EGFR inhibitor
TAS6417 is an EGFR inhibitor and an efficacious drug candidate for patients with NSCLC, with IC50 values ranging from 1.1-8.0 nM. -
EGFR inhibitor
EGFR-IN-7 (compound 34) is a selective and potent EGFR kinase inhibitor extracted from patent WO2019015655A1, has IC50s of 7.92 nM and 0.218 nM for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) respectively, and shows anti-tumor activity. -
EGFR inhibitor
Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=??1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity. -
EGFR inhibitor
Compound 56 is a cell-permeable, reversible, and ATP-competitive inhibitor of tyrosine kinase activity of EGFR. -
EGFR inhibitor
Afatinib is an irreversible EGFR/HER2 inhibitor with an IC50 of 14 nM for in vitro potency against HER2. -
EGFR inhibitor
Erlotinib mesylate is a directly acting inhibitor of human EGFR tyrosine kinase with an IC50 of 2 nM. -
EGFR Inhibitor
Gefitinib hydrochloride is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. Therefore, it is only effective in cancers with mutated and overactive EGFR. -
VEGFR/EGFR inhibitor
Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM. -
EGFR inhibitor
AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively. -
EGFR inhibitor
AZD3759 is an orally available inhibitor of the epidermal growth factor receptor (EGFR). It binds to and inhibits the activity of EGFR as well as certain mutant forms of EGFR. -
EGFR/HER2 dual inhibitor
Pyrotinib Racemate is the racemate of Pyrotinib. Pyrotinib is a potent and selective EGFR/HER2 dual inhibitor. -
EGFR inhibitor
Tyrphostin AG-528, also known as Tyrphostin B66, is a EGFR protein tyrosine kinase inhibitor. -
EGFR inhibitor
Lavendustin A is a selective inhibitor of epidermal growth factor (EGF) receptor-associated tyrosine kinase with IC50 value of 11 nM). -
EGFR inhibitor
Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively. -
c-kit/VEGFR/PDGFR Inhibitor
Famitinib is a potent multi-targeted kinase inhibitor that primarily targets c-kit, VEGFR-2, and PDGFRβ, with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively. This orally active compound demonstrates significant antitumor activity in human gastric cancer cells and xenograft models. Famitinib also induces apoptosis, making it a valuable tool for research in cancer therapeutics and signaling pathways. -
EGFR Inhibitor
EGFR-IN-86 is a potent EGFR inhibitor, exhibiting an IC50 of 1.5 nM. It demonstrates significant biological activity against glioblastoma by inducing apoptosis and causing cell cycle arrest in the G2/M phase in U87 cells. This compound serves as a valuable tool for research focused on targeting EGFR in cancer therapy. -
EGFR/HER2/TS Inhibitor
EGFR/HER2/TS-IN-1 is a selective inhibitor targeting EGFR, HER2, and thymidylate synthase (TS) with IC50 values of 0.203 μM, 0.088 μM, and 0.168 μM, respectively. This compound is effective in inducing apoptosis in MCF7 breast cancer cells, making it a valuable tool for cancer research. Its ability to simultaneously inhibit multiple targets renders it a promising candidate for exploring therapeutic strategies in malignancies characterized by overactive EGFR and HER2 signaling pathways. -
EGFR Inhibitor
EGFR-IN-150 is a potent inhibitor of the epidermal growth factor receptor (EGFR), effectively blocking phosphorylation of mutant EGFR and downstream AKT signaling, leading to antitumor activity. This compound demonstrates an IC50 of 0.386 μM in the non-small cell lung cancer (NSCLC) cell line H1975, significantly reducing colony formation and migration in both H1975 and A549 cells while promoting apoptosis. Furthermore, EGFR-IN-150 exhibits substantial tumor growth suppression in the H1975 cell-derived xenograft (CDX) mouse model, making it a valuable tool for research focused on non-small cell lung cancer. -
EGFR Inhibitor
Erbstatin is an inhibitor of the epidermal growth factor receptor (EGFR), targeting its kinase activity to impede downstream signaling pathways. This compound exhibits significant antineoplastic properties, making it a valuable reagent in cancer research. Erbstatin is utilized in studies investigating the role of EGFR in tumor progression and response to therapy, providing insights into potential treatment strategies for EGFR-mediated malignancies. -
EGFR2 Inhibitor
EGFR-IN-105 is a selective inhibitor of the EGFR2 receptor, with an IC50 value of 0.68 μM. This compound demonstrates significant anticancer activity by inducing apoptosis in cancerous cells, making it a valuable tool for investigating therapeutic strategies in pancreatic cancer research. Its specificity and potency position it as an important reagent for studies focused on targeting EGFR-related pathways in oncology. -
EGFR Inhibitor
EGFR-IN-45 is a potent inhibitor of the epidermal growth factor receptor (EGFR) with IC50 values of 0.4 µM for EGFR and 1.6 µM for CDK2. Additionally, it demonstrates inhibitory activity against Topoisomerase I and Topoisomerase II. This compound effectively induces apoptosis and arrests cancer cells in the pre-G1 phase, making it a valuable tool for cancer research and therapeutic studies targeting EGFR-related pathways. -
EGFR Inhibitor
Avitinib maleate dihydrate is a potent, irreversible, orally active selective inhibitor of epidermal growth factor receptor (EGFR). It exhibits high affinity, with IC50 values of 0.18 nM for both EGFR L858R and EGFR T790M mutations, as well as 7.68 nM for wild-type EGFR. In addition to its EGFR inhibition, Avitinib maleate dihydrate functions as a Bruton’s tyrosine kinase (BTK) inhibitor, promoting apoptosis in mantle cell lymphoma by inhibiting BTK phosphorylation. Its diverse targeting capabilities make it valuable for cancer research applications. -
EGFR Inhibitor
EGFR-IN-51 is a potent inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 0.493 µM for wild-type EGFR, 102.60 µM for the L858R-TK mutation, and 461.63 µM for the T790M-TK mutation. This compound demonstrates significant cytotoxic activity against various cancer cell lines, effectively inducing apoptosis. EGFR-IN-51 is applicable in research focused on targeted cancer therapies and elucidating the role of EGFR signaling in tumorigenesis. -
EGFR Inhibitor
EGFR-IN-141 is a potent inhibitor of the epidermal growth factor receptor (EGFR), demonstrating an IC50 of 2.67 nM. This compound exhibits significant cytotoxicity in A549 lung cancer cells, with an IC50 of 13.75 μM. EGFR-IN-141 has been shown to induce apoptosis and cause mitochondrial membrane depolarization, highlighting its potential for antitumor efficacy in cancer research applications.
