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编 号:F640874
分子式:C27H27F3N8O
分子量:536.55
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
XMU-MP-3 is a potent non-covalent BTK inhibitor with IC50s of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation in the presence of 10 μM ATP, respectively. XMU-MP-3 also induces apoptosis.

体内研究:
XMU-MP-3 (25 and 50 mg/kg) substantially suppresses tumor growth in mouse xenograft models.Animal Model:Nu/nu BALB/c mice (4-6 weeks of age) bearing BTK-transformed Ba/F3 and Ramos xenograft models
Dosage:25 and 50 mg/kg
Administration:Treated by tail vein injection; the injection volume was 0.1 mL per 10 g; daily for 14 days
Result:Significantly reduced the tumor size without affecting animal weights.

体外研究:
XMU-MP-3 (0.001-10000 nM; 48 hours) inhibits BTK-transformed Ba/F3 cell proliferation with an IC50 of 11.4 nM.XMU-MP-3 (1-10000 nM) inhibits the proliferation of JeKo-1, Ramos and NALM-6 with IC50 values of 326.6 nM, 685.6 nM and 1065 nM, respectively.XMU-MP-3 (0.001-10000 nM) maintains inhibitory potency with an IC50 of 182.3 nM against BTK(C481S)-Ba/F3 cells.XMU-MP-3 (5000 nM) induces apoptosis in BTK (C481S) Ba/F3 cells.XMU-MP-3 (10-1000 nM; 4 hours) inhibits both the auto- and trans-phosphorylation of BTK at the site of Y223 and Y551 in a dose-dependent manner in BTK-transformed Ba/F3 cells.
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