产品
编 号：F741302
分子式：C41H42FN5O7
分子量：735.8
分子式：C41H42FN5O7
分子量：735.8
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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25mg
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结构图
CAS No: 1855860-24-0
产品详情
生物活性：
DS-1205b free base is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205b free base also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo.
体内研究：
DS-1205b (3.1-50 mg/kg; p.o. bid for 5 d) exhibits pAXL inhibition mediated antitumor effects in mice.Animal Model:Female NOD/Shi-scid IL-2Rγ KO Jic mice were implanted with NIH3T3-AXL tumor blocks
Dosage:3.1, 6.3, 13, 25, 50 mg/kg
Administration:P.o. twice daily for 5 days
Result:Inhibited tumor growth by 39-94%.Reduced the phosphorylation of both AXL and AKT in tumors.
体外研究：
DS-1205b (0.3-33 μM; 2-24 h) inhibits hGAS6-induced migration in NIH3T3-AXL cells (EC50=2.7 nM).DS-1205b (1-10000 μM; 2-24 h) significantly inhibits the phosphorylation of AXL in NIH3T3-AXL cells. DS-1205b decreases NIH3T3 cell proliferation but not obviously inhibits growth (GI50>10,000 nM).
DS-1205b free base is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205b free base also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo.
体内研究：
DS-1205b (3.1-50 mg/kg; p.o. bid for 5 d) exhibits pAXL inhibition mediated antitumor effects in mice.Animal Model:Female NOD/Shi-scid IL-2Rγ KO Jic mice were implanted with NIH3T3-AXL tumor blocks
Dosage:3.1, 6.3, 13, 25, 50 mg/kg
Administration:P.o. twice daily for 5 days
Result:Inhibited tumor growth by 39-94%.Reduced the phosphorylation of both AXL and AKT in tumors.
体外研究：
DS-1205b (0.3-33 μM; 2-24 h) inhibits hGAS6-induced migration in NIH3T3-AXL cells (EC50=2.7 nM).DS-1205b (1-10000 μM; 2-24 h) significantly inhibits the phosphorylation of AXL in NIH3T3-AXL cells. DS-1205b decreases NIH3T3 cell proliferation but not obviously inhibits growth (GI50>10,000 nM).
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