DS-1205b free base

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

DS-1205b free base  纯度: 99.92%

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。

DS-1205b free base

DS-1205b free base Chemical Structure

CAS No. : 1855860-24-0

规格 价格 是否有货 数量
5 mg ￥5500 In-stock
10 mg ￥9500 In-stock
25 mg ￥19500 In-stock
50 mg ￥32500 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

DS-1205b free base 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Neuronal Signaling Compound Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Covalent Screening Library
  • Anti-Lung Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

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[1].

IC50 & Target[1]

AXL

1.3 nM (IC50)

MER

63 nM (IC50)

MET

104 nM (IC50)

TrkA

407 nM (IC50)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

735.80

Formula

C41H42FN5O7
CAS 号

1855860-24-0
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
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (67.95 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务