DC Chemicals supplies: CL-387785,cas: 194423-06-8,Catalog: DC7668,In stock.
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Product name: CL-387785, Synonyms: EKI-785; WAY-EKI 785; CL387785; CL 387785; EKI785; WAY-EKI785; EKI 785,CL-387,785, cas: 194423-06-8, MW: 381.23, Molecule Formula: C18H13BrN4O
CL-387785, cas: 194423-06-8, EKI-785; WAY-EKI 785; CL387785; CL 387785; EKI785; WAY-EKI785; EKI 785, Purity:>98%. Best Price and high quality from DC Chemicals. CL-387785(EKI785; WAY-EKI 785) is an irreversible inhibitor of EGFR with IC50 of 370+/-120 pM; is able to overcome resistance caused by the T790M mutation on a functional level.
CL-387785(EKI785; WAY-EKI 785) is an irreversible inhibitor of EGFR with IC50 of 370+/-120 pM; is able to overcome resistance caused by the T790M mutation on a functional level.
IC50 value: 370+/-120 pM
Target: EGFR
in vitro: CL-387785 blocked EGF-stimulated autophosphorylation of the receptor in cells (ic50 approximately 5 nM), inhibited cell proliferation (IC50 = 31-125 nM) primarily in a cytostatic manner in cell lines that overexpress EGF-R or c-erbB-2. Whereas trans Formation by most EGFR mutants confers on cells sensitivity to erlotinib and gefitinib, trans Formation by an exon 20 insertion makes cells resistant to these inhibitors but more sensitive to the irreversible inhibitor CL-387,785. CL-387,785 is able to overcome resistance caused by the T790M mutation on a functional level, correlating with effective inhibition of downstream signaling pathways.
in vivo: CL-387785 profoundly blocked the growth of a tumor that overexpresses EGF-R in nude mice (when given orally at 80 mg/kg/day For 10 days, daily). Treatment of BPK mice with EKI-785 resulted in a marked reduction of collecting tubule (CT) cystic lesions, improved renal function, decreased biliary epithelial abnormalities, and an increased life span. Cystic animals treated with EKI-785 to postnatal day 48 (P-48) were alive and well with normal renal function, a reduced CT cystic index of 2.0 (P < 0.02), a threefold increased in maximum urinary concentrating ability (P < 0.01), and a significant decrease in biliary epithelial proliferation/fibrosis (P < 0.01).For the detailed information of CL-387785, the solubility of CL-387785 in water, the solubility of CL-387785 in DMSO, the solubility of CL-387785 in PBS buffer, the animal experiment (test) of CL-387785, the cell expriment (test) of CL-387785, the in vivo, in vitro and clinical trial test of CL-387785, the EC50, IC50,and Affinity of CL-387785, Please contact DC Chemicals.
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