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编 号:F236707
分子式:C18H24N6O
分子量:340.42
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10mM*1mL in DMSO
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5mg
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10mg
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50mg
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100mg
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生物活性:
Bohemine is a purine analogue and is a synthetic and selective CDK inhibitor with IC50s of 4.6 μM, 83 μM, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Bohemine also inhibits ERK2 with an IC50 of 52 μM and has less inhibitory effect on CDK1, CDK4 and CDK6. Bohemine has a broad spectrum anti-cancer activities.

体内研究:
Bohemine (50 mg/kg; intravenous injection; BALB/c mice) treatment shows Cmax is 72,308 nM, observed clearance is 0.23 L/h and T1/2 is 1.39 h.Animal Model:BALB/c mice bearing the colon 26 murine tumor
Dosage:50 mg/kg
Administration:Intravenous injection (Pharmacokinetic Analysis)
Result:Cmax is 72,308 nM, observed clearance is 0.23 L/h and T1/2 is 1.39 h.

体外研究:
Bohemine (0-30 μM; 72 hours; ME-750 cells) treatment inhibits cell growth. Addition of Bohemine at concentrations in the range of 1-10 μM results in a short-term arrest of growth and of monoclonal antibody production. The short-term suppression of cell functions is followed by a significant temporary increase of specific growth rate and of specific production rate.Hybridoma cells are retarded both at the G1/S boundary and at the G2/M boundary, depending on Bohemine (0-30 μM) concentration.T-lymphoblastic cell line CEM is treated by Bohemine, five proteins are found to be downregulated, namely α-enolase, triosephosphate isomerase, initiation factor 5A, and α- and β-subunits of Rho GDP-dissociation inhibitor 1. These proteins play significant roles in glycolysis, proteosynthesis, and in cytoskeleton rearrangement.Bohemine inhibits growth of human tumor cell lines with an IC50 of 27 μM.
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