产品
编 号：F140874
分子式：C25H27N7O3S2
分子量：537.66
分子式：C25H27N7O3S2
分子量：537.66
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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2mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 1370256-78-2
产品详情
生物活性：
SKLB4771 is a potent and selective Flt3 inhibitor with an IC50 value of 10 nM. SKLB4771 downregulates the phosphorylation of FLT3/STAT5/ERK, blocks cell proliferation, and induces apoptosis in tumor tissue.
体内研究：
SKLB4771 (20-100 mg/kg; i.p.; once daily; 21 d) inhibits tumor growth in vivo without significant weight loss or any other obvious signs of toxicity on mice.Pharmacokinetic Analysis of SKLB4771 in rat (40 mg/kg; i.p.)Cmax (μg/mL)T1/2 (h)AUCmax (h·μg/mL)Tmax (h)CLobs (L/h/kg)
5.3113.921.861.02.21
Animal Model:Female NOD-SCID mouse (6?7 weeks old)
Dosage:20, 40, 100 mg/kg; dissolved in 25% (v/v) PEG400 plus 5% DMSO, administered at a dose of 5 mL/kg
Administration:Intraperitoneal injection; once daily; 21 days
Result:Inhibited tumor growth by 66% and 84% at concentration of 20 mg/kg and 40 mg/kg, respectively.Resulted cell proliferation inhibition and apoptosis induction.
体外研究：
SKLB4771 (compound 20c) (72 h) inhibits FLT3-ITD-expressing MV4-11 cells with an IC50 value of 6 nM, and inhibits other cancer cells with IC50s of 3.05 μM (Jurkat), 6.25 μM (Ramos), 3.72 μM (PC-9), 6.94 μM (H292), and 8.91 μM (A431), respectively.SKLB4771 (0-300 nM; 20 h) inhibits FLT3 phosphorylation and also decreases the phosphorylation of the downstream signaling proteins STAT5 and ERK1/2 at concentrations >0.1 μM.
SKLB4771 is a potent and selective Flt3 inhibitor with an IC50 value of 10 nM. SKLB4771 downregulates the phosphorylation of FLT3/STAT5/ERK, blocks cell proliferation, and induces apoptosis in tumor tissue.
体内研究：
SKLB4771 (20-100 mg/kg; i.p.; once daily; 21 d) inhibits tumor growth in vivo without significant weight loss or any other obvious signs of toxicity on mice.Pharmacokinetic Analysis of SKLB4771 in rat (40 mg/kg; i.p.)Cmax (μg/mL)T1/2 (h)AUCmax (h·μg/mL)Tmax (h)CLobs (L/h/kg)
5.3113.921.861.02.21
Animal Model:Female NOD-SCID mouse (6?7 weeks old)
Dosage:20, 40, 100 mg/kg; dissolved in 25% (v/v) PEG400 plus 5% DMSO, administered at a dose of 5 mL/kg
Administration:Intraperitoneal injection; once daily; 21 days
Result:Inhibited tumor growth by 66% and 84% at concentration of 20 mg/kg and 40 mg/kg, respectively.Resulted cell proliferation inhibition and apoptosis induction.
体外研究：
SKLB4771 (compound 20c) (72 h) inhibits FLT3-ITD-expressing MV4-11 cells with an IC50 value of 6 nM, and inhibits other cancer cells with IC50s of 3.05 μM (Jurkat), 6.25 μM (Ramos), 3.72 μM (PC-9), 6.94 μM (H292), and 8.91 μM (A431), respectively.SKLB4771 (0-300 nM; 20 h) inhibits FLT3 phosphorylation and also decreases the phosphorylation of the downstream signaling proteins STAT5 and ERK1/2 at concentrations >0.1 μM.
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