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닐로티닙 C화학적 특성, 용도, 생산
개요
Chronic myeloid leukemia (CML), a hematological stem-cell disorder, is
definitively diagnosed by the detection of the Philadelphia chromosome, a
truncated version of chromosome 22 resulting from the reciprocal translocation
of chromosomes 9 and 22 induced by a single mutagenic event. The consequence is
the juxtaposition of two genes creating a fusion gene BCR-ABL. This gene leads to
the translation of a fusion protein with increased tyrosine kinase activity that
contributes to the pathogenesis of CML. Targeting the BCR-ABL protein has led to
the successful intervention of the disease. Now established as first-line therapy for
CML, imatinib was the first selective tyrosine kinase inhibitor of BCR-ABL. Since
imatinib only binds to an inactive conformation of the ABL kinase portion, the
conformational restrictions contribute to its selectivity.
화학적 성질
Off-White Solid
용도
Nilotinib, an orally active signal transduction inhibitor
that selectively inhibits the tyrosine kinase Bcr-Abl, was
discovered and developed by Norvartis and was launched for
the treatment of chronic myeloid leukemia (CML) in patients
with Philadelphia chromosome-positive (Ph+) disease who
are resistant or intolerant to imatinib mesilate. Additional
clinical trials are currently underway for the treatment
of acute lymphoblastic leukemia (ALL) and gastrointestinal
stromal tumors (GISTs).
정의
ChEBI: Nilotinib is a member of (trifluoromethyl)benzenes, a member of pyrimidines, a member of pyridines, a member of imidazoles, a secondary amino compound and a secondary carboxamide. It has a role as an antineoplastic agent, a tyrosine kinase inhibitor and an anticoronaviral agent.
일반 설명
Class: non-receptor tyrosine kinase Treatment: CML Elimination half-life = 17 h Protein binding >97.5%