DS-1205

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

DS-1205 是一种有效的选择性 AXL 激酶抑制剂，IC50 为 1.3 nM。 DS-1205 还抑制 MER、MET 和 TRKA，IC50 分别为 63、104 和 407 nM。 DS-1205可以抑制体外细胞迁移和体内肿瘤生长。

DS-1205 is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205 also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively. DS-1205 can inhibit cell migration in vitro and tumor growth in vivo.(In Vitro):DS-1205 (0.3-33 μM; 2-24 h) inhibits hGAS6-induced migration in NIH3T3-AXL cells (EC50=2.7 nM). DS-1205 (1-10000 μM; 2-24 h) significantly inhibits the phosphorylation of AXL in NIH3T3-AXL cells. DS-1205 decreases NIH3T3 cell proliferation but not obviously inhibits growth (GI50>10,000 nM).(In Vivo):DS-1205 (3.1-50 mg/kg; p.o. bid for 5 d) exhibits pAXL inhibition mediated antitumor effects in mice.

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). Western Blot Analysis Cell Line:NIH3T3-AXL cells Concentration:1, 10, 100, 1000, 10000 μM Incubation Time:2, 24 hours Result:Completely inhibited the phosphorylation of AXL at concentrations above 10 nM.Slightly inhibited the phosphorylation of AKT serine/threonine kinase in a dose-dependent manner.

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.

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Tyrosine Kinase

TAM Receptor

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1855860-24-0

284.32

C14H16N6O

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (67.95 mM)

Nc1nonc1-c1nc(cncc2)c2n1C1CCCCC1

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(-20℃)

With Ice Pack

≥ 2 years