Linifanib (Synonyms:ABT-869; AL-39324)
目录号 : KM16494 CAS No. : 796967-16-3 纯度 : 98%

Linifanib (ABT-869) 是一种高效、口服的 VEGFR 和 PDGFR 家族多靶点抑制剂,对 KDR、FLT1、PDGFRβ、FLT3 的 IC50s 分别为 4、3、66、4 nM。Linifanib 具有显著的抗肿瘤活性。Linifanib 对无关 RTKs、可溶性酪氨酸激酶或丝氨酸/苏氨酸激酶的活性要低得多。Linifanib 是一种特异的 miR-10b 抑制剂,阻断 miR-10b 的生物合成。

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生物活性

Linifanib (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib shows prominent antitumor activity. Linifanib has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib is a specific miR-10b inhibitor that blocks miR-10b biogenesis.

体外研究

Linifanib (0-10000 nM; 72 hours) inhibits in vitro the cell proliferation of 8305C and 8505C cell lines in a concentration-dependent manner.
Linifanib significantly decreased the levels of phospho-CSF-1R after 24 h and 72 h in both 8505C and 8305C cells.

Cell Viability Assay

Cell Line: 8305C and 8505C cells
Concentration: 0-10000 nM
Incubation Time: 72 hours
Result: Inhibited the 8305C and 8505C cell proliferation with an IC50 of 0.7 nM and 123.7 nM, respectively.
体内研究

The synergistic ATC antitumor activity of linifanib (10 mg/kg; p.o.; daily for 33 days)/Irinotecan combination significantly increases the survival of ATC affected mice and induces some complete responses.

Animal Model: Six-week-old CD nu/nu male mice (bearing 8505C ATC cells)
Dosage: 10 mg/kg
Administration: P.o.; daily for 33 days
Result: The combination of linifanib and irinotecan produced a greater survival result than either monotherapy, and resulted in a significant higher median survival of 100 days.
分子式
C21H18FN5O
分子量
375.40
CAS号
796967-16-3
中文名称
利尼伐尼
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 : 13.16 mg/mL (35.06 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6638 mL 13.3191 mL 26.6383 mL
5 mM 0.5328 mL 2.6638 mL 5.3277 mL
10 mM 0.2664 mL 1.3319 mL 2.6638 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: ≥ 1.32 mg/mL (3.52 mM); Clear solution

    此方案可获得 ≥ 1.32 mg/mL (3.52 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 13.2 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。

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.32 mg/mL (3.52 mM); Clear solution

    此方案可获得 ≥ 1.32 mg/mL (3.52 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 13.2 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 1.32 mg/mL (3.52 mM); Clear solution

    此方案可获得 ≥ 1.32 mg/mL (3.52 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 13.2 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

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