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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 inhibitor
Tyrphostin AG 183 inhibits EGFR (epidermal growth factor receptor) tyrosine kinase (IC50 = 800 nM). -
EGFR Inhibitor
EGFR inhibitor is a cell permeable, 4,6-disubstituted pyrimidine compound that selectively inhibits the EGFR kinase with an IC50 value of 21 nM in vitro and blocks receptor autophosphorylation in cells. -
EGFR inhibitor
Icotinib hydrochloride is a potent and specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with an IC(50) of 5 nM, including it's mutants of EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R). -
EGFR inhibitor
CNX-2006 is a potent, mutant-selective EGFR inhibitor with excellent in vitro activity in cells with activating EGFR mutations, as well as in cells harbouring the T790M mutation. CNX-2006 is the prototype for CO-1686, which is currently in a Phase I clinical trial for the treatment of EGFR-mutant lung cancer. -
irreversible EGFR inhibitor
ASP8273 is an orally available, irreversible, third-generation, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. -
EGFR T790M inhibitor
EGF816 is a novel covalent inhibitor of mutant-selective EGFR; overcomes T790M-mediated resistance in NSCLC. -
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 Inhibitor
EGFR-IN-47 is a potent orally active inhibitor of the EGFR L858R/T790M/C797S mutations, with an IC50 of 0.01 μM. This compound effectively induces cell cycle arrest and promotes apoptosis in cancer cells. EGFR-IN-47 holds significant potential for research applications related to non-small cell lung cancer (NSCLC). -
EGFR Inhibitor
EGFR-IN-78 is a reversible inhibitor of the EGFR variant C797S-TK, classified as a 2-aminopyrimidine derivative. This compound induces apoptosis and exhibits significant anti-proliferative activity by inhibiting EGFR phosphorylation. Additionally, EGFR-IN-78 effectively arrests the cell cycle at the G2/M phase, making it a valuable tool for research applications focused on targeted cancer therapies. -
EGFR-TK Inhibitor
EGFR-TK-IN-4 is a potent and selective inhibitor of the epidermal growth factor receptor tyrosine kinase (EGFR-TK). It has been demonstrated to induce apoptosis in cancer cells and exhibits significant antitumor activity. This compound is suitable for studying EGFR signaling pathways and developing targeted therapies in oncology research. -
EGFR Inhibitor
YS-363 is a potent and selective orally active inhibitor of the epidermal growth factor receptor (EGFR), exhibiting IC50 values of 0.96 nM for wild-type and 0.67 nM for the L858R mutant form. This compound effectively induces G0/G1 cell cycle arrest and promotes apoptosis in target cells. YS-363 is valuable for research applications focused on cancer therapeutics and the molecular mechanisms of EGFR signaling. -
EGFRC797S-TK Inhibitor
Os30 is a potent fourth-generation EGFR inhibitor specifically targeting the EGFRC797S-TK mutation. With IC50 values of 18 nM and 113 nM for EGFRDel19/T790M/C797S TK and EGFRL858R/T790M/C797S TK, respectively, Os30 effectively inhibits EGFR phosphorylation, induces G1 phase cell cycle arrest, and triggers apoptosis in KC-0116 (BaF3-EGFRDel19/T790M/C797S) cells. This compound demonstrates significant antitumor activity in non-small cell lung cancer (NSCLC) harboring the EGFRC797S mutation, making it a valuable tool for cancer research and therapeutic exploration. -
Pan-HER Inhibitor
pan-HER-IN-2 is a reversible, orally active pan-HER inhibitor targeting multiple receptor tyrosine kinases, with IC50 values of 0.72 nM for EGFR, 2.0 nM for HER4, 8.2 nM for EGFRT790M/L858R, and 75.1 nM for HER2. This compound effectively induces apoptosis and exhibits significant antitumor activities. pan-HER-IN-2 is suitable for research applications focused on cancer therapy and the exploration of targeted treatments for HER family receptor-positive tumors. -
EGFR Inhibitor
Gefitinib dihydrochloride is a potent and selective inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, exhibiting an IC50 of 33 nM. This compound effectively inhibits EGF-stimulated tumor cell proliferation (IC50 of 54 nM) and prevents EGFR autophosphorylation, thereby blocking downstream signaling pathways. Gefitinib dihydrochloride is valuable for cancer research, particularly in the study of lung and breast cancers, due to its ability to induce autophagy and promote apoptosis in tumor cells. -
EGFR Inhibitor
Zorifertinib hydrochloride is a potent orally active inhibitor of the epidermal growth factor receptor (EGFR), demonstrating IC50 values of 0.3 nM, 0.2 nM, and 0.2 nM against wild-type EGFR, EGFR L858R, and EGFR exon 19 deletion variants, respectively. This compound is capable of inducing apoptosis in cancer cells and exhibits significant antitumor activity. Zorifertinib hydrochloride is primarily utilized in research related to non-small cell lung cancer (NSCLC) and hepatocellular carcinoma (HCC).
