Nazartinib mesylate (EGF816 mesylate) is a novel, covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min?1 on EGFR(L858R/790M) mutant, respectively. 了解更多
Momelotinib Mesylate (CYT387 Mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3. 了解更多
Ghazal Nabil, .et al. CD44 Targeted Nanomaterials for Treatment of Triple-Negative Breast Cancer, Cancers (Basel), 2021, Feb 20;13(4):898 PMID: 33672756
CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. 了解更多
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. 了解更多
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. 了解更多
JAK1-IN-4 is a potent and selective JAK1 inhibitor, with IC50s of 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively. JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM). 了解更多
JAK3 covalent inhibitor-1 is a potent and selective janus kinase 3 (JAK3) covalent inhibitor with an IC50 of 11 nM and shows 246-fold selectivity vs other JAKs. 了解更多
Tyk2-IN-8 (compound 10) is a selective TYK2 inhibitor, which binds to TYK2 catalytically active JH1 domain with an IC50 of 17 nM, used in the treatment of psoriasis. 了解更多
Liu YN, .et al. Acquired resistance to EGFR tyrosine kinase inhibitors is mediated by the reactivation of STC2/JUN/AXL signaling in lung cancer, Int J Cancer, 2019, Jun 4 PMID: 31162839
Remy J, .et al. Inhibition of PIM1 blocks the autophagic flux to sensitize glioblastoma cells to ABT-737-induced apoptosis, Biochim Biophys Acta Mol Cell Res, 2019, Feb;1866(2):175-189 PMID: 30389373
Andrea L. Casillas, .et al. Hypoxia-inducible PIM kinase expression promotes resistance to anti-angiogenic agents, Clin Cancer Res, 2018, Jan 1; 24(1): 169-180 PMID: 29084916
Jin H. Song, .et al. Mechanisms Behind Resistance to PI3K Inhibitor Treatment Induced by the PIM Kinase, Mol Cancer Ther, 2018, Dec;17(12):2710-2721 PMID: 30190422
Sathish K.R. Padi, .et al. Targeting the PIM protein kinases for the treatment of a T-cell acute lymphoblastic leukemia subset, Oncotarget, 2017, May 2; 8(18): 30199-30216 PMID: 28415816
Lim R, .et al. Inhibition of PIM1 kinase attenuates inflammation-induced pro-labour mediators in human foetal membranes in vitro, Mol Hum Reprod, 2017, Jun 1;23(6):428-440 PMID: 28333279
Takeshi Ito, .et al. Mathematical analysis of gefitinib resistance of lung adenocarcinoma caused by MET amplification, Biochem Biophys Res Commun, 2019, in Press
Simona Moravcova, .et al. The Circadian Rhythms of STAT3 in the Rat Pineal Gland and Its Involvement in Arylalkylamine-N-Acetyltransferase Regulation, Life (Basel), 2021, Oct 18;11(10):1105 PMID: 34685476
JOIN OUR REWARDS PROGRAM TODAY AND START EARNING POINTS RIGHT AWAY !
Beginning Aug 26th, 2019, all customers purchasing Adooq products can earn Reward Points by collecting and registering point codes . Registered codes will be associated with your order and points will be awarded ($1 = 1 point). E.g. Orders valued at $300, will receive 300 points. Orders valued at $1000, will receive 400 points.