zm 39923 hcl is an 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.
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.
pralatrexate is a folate analogue inhibitor of dihydrofolate reductase (dhfr) exhibiting high affinity for reduced folate carrier-1 (rfc-1) with antineoplastic and immunosuppressive activities.
blz945 is an orally active, effective and specific csf-1r inhibitor (ic50: 1 nm), >1000-fold selective against its closest receptor tyrosine kinase homologs.
bleomycin sulfate, a glycopeptide antibiotic, is an anticancer agent for squamous cell carcinomas (scc). in ut-scc-19a cells, the ic50 of bleomycin sulfate is 4 nm.
doxercalciferol is a synthetic vitamin d2 analog, suppressing parathyroid synthesis and secretion, used to treat secondary hyperparathyroidism and metabolic bone disease.
cerdulatinib (prt-062070) is an oral active, multi-targeted tyrosine kinase inhibitor with ic50 of 12 nm/6 nm/8 nm/0.5 nm and 32 nm for jak1/jak2/jak3/tyk2 and syk, respectively. also inhibits 19 other tested kinases with ic50 less than 200 nm.
torin 2(ic50=0.25 nm), a specific and effective mtor inhibitor, is the 800-fold greater specific activity for mtor than pi3k and improves pharmacokinetic properties. the ec50 of torin 2 for atm/atr/dna-pk inhibition is 28 nm/35 nm/118 nm, respectively.
cabotegravir (gsk744, gsk1265744) is a long-acting hiv integrase inhibitor and inhibits the hiv-1 integrase catalyzed strand transfer reaction (ic50: 3.0 nm).
azd7762, an effective and specific inhibitor of chk1��ic50=5 nm��, is equally potent against chk2 and less potent against cam, yes, fyn, lyn, hck and lck.
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.
cp-673451 is a specific inhibitor of pdgfr��/�� (ic50: 10/1 nm) with antiangiogenic and antitumor activity and the selectivity is higher 450-fold than other angiogenic receptors.