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。
| 生物活性 | DS-1205b free base is a potent and selective inhibitor ofAXL kinase, with anIC50of 1.3 nM. DS-1205b free base also inhibitsMER,MET, andTRKA, withIC50s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo[1]. |
| IC50& Target[1] | AXL 1.3 nM (IC50) | MER 63 nM (IC50) | TrkA 407 nM (IC50) | Met 104 nM (IC50) |
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体外研究
(In Vitro) | 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].
Western Blot Analysis[1] | 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. |
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体内研究
(In Vivo) | DS-1205b (3.1-50 mg/kg; p.o. bid for 5 d) exhibits pAXL inhibition mediated antitumor effects in mice[1].
| Animal Model: | Female NOD/Shi-scid IL-2Rγ KO Jic mice were implanted with NIH3T3-AXL tumor blocks[1] | | 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(67.95 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.3591 mL | 6.7953 mL | 13.5907 mL | | 5 mM | 0.2718 mL | 1.3591 mL | 2.7181 mL | | 10 mM | 0.1359 mL | 0.6795 mL | 1.3591 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (3.40 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.40 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 *以上所有助溶剂都可在本网站选购。
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