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PI-103 hydrochloride说明

发布日期:2018-04-24   浏览次数:0
核心提示:PI-103 hydrochloride是有效地PI3K/Akt and mTOR抑制剂,对重组PI3K同工型p110α和mTOR的IC50值分别为2 nM和30 nM。
PI-103 hydrochloride是有效地PI3K/Akt and mTOR抑制剂,对重组PI3K同工型p110α和mTOR的IC50值分别为2 nM和30 nM。
Mizoribine产品描述:Mizoribine(NSC 289637; HE 69; β-Bredinin) is an immunosuppressive agents (IC50=100 uM) that inhibit the proliferation of lymphocytes selectively, via inhibition of IMPDH. IC50 Value: Target: IMPDH in vitro: Unlike azathioprine, Mizoribine is not taken up by nucleic acids in the cell. Instead, after phosphorylation MZR-5 -monophosphate inhibits GMP synthesis by the antagonistic blocking of IMPDH (Ki = 10(-8)M) and GMP- synthetase (Ki =10(-5) M) [1]. Pretreatment of cells with MZR partially, but significantly, attenuates the expression of monocyte chemoattractant protein (MCP)-1 mRNA and protein, wheras the poly IC-induced expressions for the other functional molecules, such as CCL5, fractalkine and IL-8 were not influenced by MZR treatment [2]. in vivo:MZR 150 mg was administered once a day. After 6 months, the remission rate was 72.7% (2 subjects achieved complete remission, and 9 partial remission). After 3 and 6 months, significant reductions (p < 0.01) were obtained in 24-h pr


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Purity:98%
MWt:384.8163
Formula:C19H17ClN4O3
SMILES:OC1=CC(C2=NC3=C(OC4=C3C=CC=N4)C(N5CCOCC5)=N2)=CC=C1.[H]Cl
Pathway:PI3K/Akt/mTOR;
Mechanisms:mTOR; PI3K;
Research Area:Cancer
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关键词: PI-103 hydrochloride