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Volumn 21, Issue 2, 2011, Pages 781-785

Novel pyrrolo[2,1-f][1,2,4]triazin-4-amines: Dual inhibitors of EGFR and HER2 protein tyrosine kinases

Author keywords

EGFR; HER2; Kinase inhibitor

Indexed keywords

5 [(4 AMINOPIPERIDIN 1 YL)METHYL]PYRROLO[2,1 F][1,2,4]TRIAZIN 4 AMINE DERIVATIVE; EPIDERMAL GROWTH FACTOR RECEPTOR 2; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; UNCLASSIFIED DRUG;

EID: 78651250889     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.11.100     Document Type: Article
Times cited : (28)

References (19)
  • 15
    • 0141599428 scopus 로고    scopus 로고
    • Molsoft modeling software was used to produce this figure. Molsoft LLC, 3366 No. Torrey Pines Ct., Ste. 300, La Jolla, CA 92037
    • Stamos, J.; Slikowski, C.; Eigenbrot, C. J. Biol. Chem. 2002, 277, 46,265. Molsoft modeling software was used to produce this figure. Molsoft LLC, 3366 No. Torrey Pines Ct., Ste. 300, La Jolla, CA 92037.
    • (2002) J. Biol. Chem. , vol.277 , Issue.46 , pp. 265
    • Stamos, J.1    Slikowski, C.2    Eigenbrot, C.3
  • 16
    • 84855627142 scopus 로고    scopus 로고
    • 6) δ 9.6 (s, 1H, NH)
    • 6) δ 9.6 (s, 1H, NH).
  • 18
    • 84855627252 scopus 로고    scopus 로고
    • The free fraction (fu) for 8l and 3 were 1.2% and 2.6%, respectively, as determined by equilibrium dialysis at 10 μM
    • The free fraction (fu) for 8l and 3 were 1.2% and 2.6%, respectively, as determined by equilibrium dialysis at 10 μM.
  • 19
    • 78651252147 scopus 로고    scopus 로고
    • note
    • Tumors were excised and homogenized in a glass homogenizer using a buffer that contained 1% Triton X-100, 40 mM Tris-HCl (pH 7.7), 10% glycerol, 1 mM EDTA, 0.15 M NaCl, 1 mM sodium vanadate, and 40 μM ammonium molybdate. Tumor lysates were centrifuged at 12,000×g for 10 min and the supernatants were saved. Since the HER2 gene is amplified in N87 tumors, receptor phosphorylation was readily quantitated by western blot analyzes using tumor lysates directly. Tumor lysates (50 μg proteins) were fractionated by gel electrophoresis and western blot analysis was carried out using anti-phosphotyrosine antibody (PY20, Invitrogen), and anti-HER2 antibody (see Ref. 4b). HER2 receptor phosphorylation was quantified by densitometry and normalized against HER2 receptor levels.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.