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  • DS-1205b free base
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DS-1205b free base

DS-1205b free base 是一种有效和选择性的 AXL 激酶抑制剂,IC50 值为 1.3 nM。DS-1205b free base 还可以抑制 MER,MET 和 TRKA,IC50 值分别为 63、104 和 407 nM。 DS-1205b free base 可以抑制细胞迁移和肿瘤生长。

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DS-1205b free base的二维码
  • 库存: 现货
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  • 5mg
    ¥5937.00
    4750.00
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  • 10mg
    ¥10250.00
    8200.00
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  • 25mg
    ¥20837.00
    16670.00
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  • 50mg
    ¥34725.00
    27780.00
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  • 货号: ajcx34038
  • CAS: 1855860-24-0
  • 别名:
  • 分子式: C41H42FN5O7
  • 分子量: 735.8
  • 纯度: >98%
  • 溶解度: DMSO : 50 mg/mL (67.95 mM; Need ultrasonic)
  • 储存: Store at -20°C
  • 库存: 现货

Background

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[1].


DS-1205b (0.3-33 μM; 2-24 h) inhibits hGAS6-induced migration in NIH3T3-AXL cells (EC50=2.7 nM)[1].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)[1].


DS-1205b (3.1-50 mg/kg; p.o. bid for 5 d) exhibits pAXL inhibition mediated antitumor effects in mice[1].


[1]. Jimbo T, et, al. DS-1205b, a novel selective inhibitor of AXL kinase, blocks resistance to EGFR-tyrosine kinase inhibitors in a non-small cell lung cancer xenograft model. Oncotarget. 2019 Aug 27;10(50):5152-5167.

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