Bosutinib(Synonyms: SKI-606) | 赛默飞Alfa aesar官网

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Bosutinib (Synonyms: SKI-606) 纯度: 99.89%

Bosutinib是 Src/Abl 的双抑制剂， IC₅₀ 分别为1.2 nM和1 nM。

Bosutinib Chemical Structure

CAS No. : 380843-75-4

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10 mM * 1 mL in DMSO	￥500	In-stock
10 mg	￥450	In-stock
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100 mg	￥1100	In-stock
200 mg	￥1800	In-stock
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1 g		询价

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生物活性

Bosutinib is a dual Src/Abl inhibitor with IC₅₀s of 1.2 nM and 1 nM, respectively.

IC₅₀ & Target

IC50: 1.2 nM (Src), 1 nM (Abl)^[1]

体外研究
(In Vitro)

Bosutinib (100 nM; 24/48 hours) results in a reduction of S and G2-M phase cells and an increase of cells with a DNA content of less than 2N^[3].
Bosutinib inhibits the proliferation of all three cell lines, with IC₅₀s ranging from 5 nM in the KU812 line to 20 nM for the K562 and MEG-01 cell lines^[3].
Bosutinib (10-500 nM; 4 hours) ablates tyrosine phosphorylation of STAT5 at 25 nM^[3].

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.

Cell Cycle Analysis^[3]

Cell Line:	KU812, K562 cells
Concentration:	100 nM
Incubation Time:	24 hours (KU812 cells), 48 hours (K562 cells)
Result:	Resulted in a reduction of S and G2-M phase cells and an increase of cells with a DNA content of less than 2N.

Western Blot Analysis^[3]

Cell Line:	K562 cells
Concentration:	10 nM, 25 nM, 50 nM, 100 nM, 500 nM
Incubation Time:	4 hours
Result:	Tyrosine phosphorylation of STAT5 was ablated by 25 nM.

体内研究
(In Vivo)

Bosutinib (50-150 mg; p.o.; once a day for 5 days) remaines tumor free at 150 mg/kg, whereas at the lower doses, some relapse occurs over a 40-day period in K562 Xenografts in Nude Mice^[3].

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:	Nude female mice 6–7 weeks of age (K562 xenografts)^[3]
Dosage:	50, 75, 100, 150 mg/kg
Administration:	Oral administration, once a day for 5 days
Result:	Remained tumor free at 150 mg/kg, whereas at the lower doses, some relapse occurred over a 40-day period.

Clinical Trial

分子量

530.45

Formula

C₂₆H₂₉Cl₂N₅O₃

CAS 号

380843-75-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

In Vitro:

DMSO : ≥ 46 mg/mL (86.72 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8852 mL	9.4260 mL	18.8519 mL
5 mM	0.3770 mL	1.8852 mL	3.7704 mL
10 mM	0.1885 mL	0.9426 mL	1.8852 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 (protect from light)。-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 (4.71 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.71 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
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.71 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.71 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
3.

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

Solubility: ≥ 2.08 mg/mL (3.92 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.92 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 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。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*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]. Boschelli DH, et al. Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity. J Med Chem, 2001, 44(23), 3965-3977.

[2]. Golas JM, et al. SKI-606, a 4-anilino-3-quinolinecarbonitrile dual inhibitor of Src and Abl kinases, is a potent antiproliferative agent against chronic myelogenous leukemia cells in culture and causes regression of K562 xenografts in nude mice. Cancer Res, 2003, 63(2), 375-381.

[3]. Vultur A, et al. SKI-606 (bosutinib), a novel Src kinase inhibitor, suppresses migration and invasion of human breast cancer cells. Mol Cancer Ther, 2008, 7(5), 1185-1194.

[4]. Golas JM, et al. SKI-606, a Src/Abl inhibitor with in vivo activity in colon tumor xenograft models. Cancer Res, 2005, 65(12), 5358-5364.

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