Bosutinib 伯舒替尼；博舒替尼；博苏替尼

目录号 M1685 所有产品仅供科研使用，严禁用于人或动物的治疗等任何其他用途，不为任何个人提供产品和服务

Bosutinib (SKI-606)是一种新型的Sarcoma/Abelson (Src/Abl)酪氨酸激酶双重抑制剂，其IC50分别为1.2 nM和1 nM。

别名：SKI-606

规格	价格	库存状态
Free Sample (0.5-1 mg)	¥ 0	中国库存现货
10mg	¥ 440	中国库存现货
50mg	¥ 840	中国库存现货
100mg	¥ 1080	中国库存现货

其他规格数量报价？

质量标准及产品资料

纯度： >99%
COA
MSDS

产品信息

生物活性

Bosutinib (SKI-606)是一种新型的Sarcoma/Abelson (Src/Abl)酪氨酸激酶双重抑制剂，其IC50分别为1.2 nM和1 nM。Bosutinib作用于Src比非Src家族激酶选择性高，IC50为1.2 nM,且有效抑制Src依赖的细胞增殖，IC50为100 nM。 Bosutinib 显著抑制Bcr-Abl阳性白血病细胞系KU812, K562, 和MEG-01 而不是 Molt-4, HL-60, Ramos, 和其他白血病细胞系的增殖，IC50分别为5 nM, 20 nM,和20 nM，比 STI-571更有效。与STI-571类似, Bosutinib 作用于Abl-MLV转化纤维，具有看增殖活性，IC50为 90 nM。

使用AbMole产品发表的文献

J Virol. 2020 Feb 14;94(5):e01791-19.

Targeting Kaposi's Sarcoma-Associated Herpesvirus ORF21 Tyrosine Kinase and Viral Lytic Reactivation by Tyrosine Kinase Inhibitors Approved for Clinical Use

实验参考

体外实验*
细胞系	Abl-MLV, Rat 2, MEG-01, and K562 cell lines
方法	cell lines were obtained from the American Type Culture Collection. The KU812 line was obtained from the European Collection of Cell Cultures. K562 and KU812 cell lines were maintained in RPMI 1640 supplemented with 10% FCS, glutamine, and nonessential amino acids (Life Technologies, Inc.). Rat 2 and Abl-MLV-transformed Rat 2 cells were maintained in high-glucose DMEM supplemented with 10% FCS. For proliferation assays, cells were exposed to compound for 72 h, and relative proliferation was measured with either 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxy-phenyl)-2-(4-sulfonyl)-2H-tetrazolium (Promega) or Cell-Glo (Promega). Anchorage-independent proliferation of Abl-MLV-transformed fibroblasts was measured in 96-well ultra-low binding plates (Costar) treated with Sigmacote (Sigma) to block residual cell attachment. Data analysis for IC50 calculations was performed with the LSW Data Analysis Package plug-in for Excel (Microsoft). For biochemical assays, cells were incubated with compound or DMSO alone for 4 h. Cells were prepared for FACS analysis as described in the CycleTest Plus DNA reagent kit (Becton Dickinson) and analyzed on a fluorescence-activated cell sorter flow cytometer.
浓度	0~1µM
处理时间	72h

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

体内实验*
动物模型	K562 Xenografts in nude mice
配制	in a 0.2-ml suspension with 0.5% methocel/0.4% Tween 80.
剂量	75 mg/kg twice a day
给药处理	oral gavage

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

化学性质

分子量	530.45
分子式	C26H29Cl2N5O3
CAS号	380843-75-4
溶解性（25°C）	DMSO
储存条件	2-8°C, protect from light
运输方式	冰袋运输，根据产品的不同，可能会有相应调整。

储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.8852 mL	9.426 mL	18.8519 mL
5 mM	0.377 mL	1.8852 mL	3.7704 mL
10 mM	0.1885 mL	0.9426 mL	1.8852 mL

不同实验动物依据体表面积的等效剂量转换表（参考来源于公开文献）

	小鼠	大鼠	兔	豚鼠	仓鼠	狗
重量 (kg)	0.02	0.15	1.8	0.4	0.08	10
体表面积 (m²)	0.007	0.025	0.15	0.05	0.02	0.5
K_m 系数	3	6	12	8	5	20

动物 A (mg/kg) = 动物 B (mg/kg) ×	动物 B的K_m系数
	动物 A的K_m系数

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Cortes et al. J Clin Oncol. Bosutinib Versus Imatinib in Newly Diagnosed Chronic-Phase Chronic Myeloid Leukemia: Results From the BELA Trial.

[2] Abbas et al. Clin Ther. Ascending Single-Dose Study of the Safety Profile, Tolerability, and Pharmacokinetics of Bosutinib Coadministered With Ketoconazole to Healthy Adult Subjects.

[3] Levinson et al. PLoS One. Structural and spectroscopic analysis of the kinase inhibitor bosutinib and an isomer of bosutinib binding to the Abl tyrosine kinase domain.

[4] Quintás-Cardama et al. Drugs Today (Barc), Bosutinib for the treatment of chronic myeloid leukemia in chronic phase.

[5] Khoury et al. Blood. Bosutinib is active in chronic phase chronic myeloid leukemia after imatinib and dasatinib and/or nilotinib therapy failure.

[6] Kim et al. Clin Cancer Res. SKI-606, an Src inhibitor, reduces tumor growth, invasion, and distant metastasis in a mouse model of thyroid cancer.

[7] Daud et al. Clin Cancer Res. Phase I study of bosutinib, a src/abl tyrosine kinase inhibitor, administered to patients with advanced solid tumors.

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