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伯舒替尼

伯舒替尼用途

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

伯舒替尼名称

[ CAS 号 ]:
380843-75-4

[ 中文名 ]:
伯舒替尼

[ 英文名 ]:
Bosutinib (SKI-606)

[中文别名 ]:

[英文别名 ]:

Bosutinib(SKI 606)
SKI 606
SKI-606
Bosutinib
Bosutinib for research
Bosutinib (SKI-606)
T66 BNJ DCN EMR BG DG EO1& HO1 IO3- AT6N DNTJ D1

伯舒替尼生物活性

[ 描述 ]:

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

[ 相关类别 ]:

信号通路 >> 蛋白酪氨酸激酶 >> BCR-ABL

信号通路 >> 蛋白酪氨酸激酶 >> SRC

研究领域 >> 癌症

[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.

[相关活性小分子]

伯舒替尼物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
649.7±55.0 °C at 760 mmHg

[ 熔点 ]:
116-120ºC

[ 分子式 ]:
C₂₆H₂₉Cl₂N₅O₃

[ 分子量 ]:
530.446

[ 闪点 ]:
346.7±31.5 °C

[ 精确质量 ]:
529.164734

[ PSA ]:
82.88000

[ LogP ]:
5.48

[ 蒸汽压 ]:
0.0±1.9 mmHg at 25°C

[ 折射率 ]:
1.652

[ 储存条件 ]:
room temp

伯舒替尼MSDS

伯舒替尼安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H319-H413

[ 警示性声明 ]:
P305 + P351 + P338

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
36

[ 安全声明 (欧洲) ]:
26

[ 危险品运输编码 ]:
NONH for all modes of transport

伯舒替尼合成路线

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伯舒替尼文献

Src Kinase Is the Connecting Player between Protein Kinase A (PKA) Activation and Hyperpolarization through SLO3 Potassium Channel Regulation in Mouse Sperm.

J. Biol. Chem. 290 , 18855-64, (2015)

Plasma membrane hyperpolarization is crucial for mammalian sperm to acquire acrosomal responsiveness during capacitation. Among the signaling events leading to mammalian sperm capacitation, the immedi...

In vitro and in vivo identification of ABCB1 as an efflux transporter of bosutinib.

J. Hematol. Oncol. 8 , 81, (2015)

Bosutinib is a recently approved ABL inhibitor. In spite of the well-documented effectiveness of BCR-ABL inhibitors in treating chronic myeloid leukemia, development of resistance is a continuous clin...

A simple method for the determination of Bosutinib in rat plasma by UPLC-MS/MS.

J. Chromatogr. B. Analyt. Technol. Biomed. Life Sci. 1004 , 93-7, (2015)

In this work, a simple, sensitive and fast ultra performance liquid chromatography with tandem mass spectrometry (UPLC-MS/MS) method was developed and validated for the quantitative determination of b...

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伯舒替尼相关知识

伯舒替尼的生物活性和实验方法

2018-10-23 11:47:42

伯舒替尼是一种合成的喹诺酮衍生物和双激酶抑制剂，可靶向具有潜在抗肿瘤活性的Abl和Src激酶。伯舒替尼抑制Abl和Src激酶的自身磷酸化，导致细胞生长和细胞凋亡的抑制。一、伯舒替尼的生物活性详解：1）体外活性伯舒替尼对Src的选择性高于非Src家族激酶，IC50为1.2 nM，有效抑制Src依赖...

伯舒替尼

伯舒替尼用途

伯舒替尼名称

伯舒替尼生物活性

伯舒替尼物理化学性质

伯舒替尼MSDS

详细MSDS(安全技术说明书)

伯舒替尼安全信息

伯舒替尼合成路线

详细合成路线

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伯舒替尼文献

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