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博舒替尼 /Bosutinib {[allProObj[0].p_purity_real_show]}

货号:A730879 同义名: 伯舒替尼 (SKI-606) / SKI-606

Bosutinib is an inhibitor of Src and Abl with IC50 of 1.2 nM and 1 nM.

Bosutinib 化学结构 CAS号:380843-75-4
Bosutinib 化学结构
CAS号:380843-75-4
Bosutinib 3D分子结构
CAS号:380843-75-4
Bosutinib 化学结构 CAS号:380843-75-4
Bosutinib 3D分子结构 CAS号:380843-75-4
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Bosutinib 纯度/质量文件 产品仅供科研

货号:A730879 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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产品名称 Fyn Lck Lyn Src Yes 其他靶点 纯度
Saracatinib ++

Fyn, IC50: 10 nM

++++

LCK, IC50: <4 nM

+++

Lyn, IC50: 5 nM

++++

c-Src, IC50: 2.7 nM

99%+
SU6656 +

Fyn, IC50: 170 nM

+

Lyn, IC50: 130 nM

+

Src, IC50: 280 nM

++

YES, IC50: 20 nM

98%
PP1 +++

Fyn, IC50: 6 nM

+++

LCK, IC50: 5 nM

EGFR 99%+
PP2 +++

Fyn, IC50: 5 nM

++++

LCK, IC50: 4 nM

98%
WH-4-023 ++++

Lck, IC50: 2 nM

+++

Src, IC50: 6 nM

99%+
NVP-BHG 712 +

c-Src, IC50: 1.266 μM

99%+
CCT196969 ++

LCK, IC50: 0.02 μM

+

Src, IC50: 0.03 μM

98%
MNS +

Src, IC50: 29.3 μM

p97,Syk 98%
Tirbanibulin ++

Src (HuH7), GI50: 13 nM

Src (Hep 3B), GI50: 26 nM

99%+
PP121 ++

Src, IC50: 14 nM

PDGFR,VEGFR 99%+
Bosutinib ++++

Src, IC50: 1.2 nM

99%
Dasatinib monohydrate ++++

Src, IC50: 0.8 nM

98%
Quercetin Sirtuin,PKC 97%
Dasatinib ++++

Src, IC50: 0.8 nM

98%
Repotrectinib +++

Src, IC50: 5.3 nM

99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Bosutinib 生物活性

靶点
  • Src

    Src, IC50:1.2 nM

描述 Bosutinib is an orally active inhibitor of Src/Abl tyrosine kinases, with IC50 values of 1.2 nM and 1 nM, respectively[1]. Bosutinib is an active inhibitor of Bcr-Abl in various chronic myelogenous leukemia cell lines, with IC50 values in the low nanomolar range[2].

Bosutinib 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
23132-87 Growth Inhibition Assay IC50=15.8495 μM SANGER
5637 Growth Inhibition Assay IC50=1.13803 μM SANGER
647-V Growth Inhibition Assay IC50=29.7003 μM SANGER
697 Growth Inhibition Assay IC50=0.45633 μM SANGER

Bosutinib 动物研究

Animal study Bosutinib, administered via oral gavage at a dose of 75 mg/kg twice daily, or 150 mg/kg once daily, is active against human KU812 xenografts in nude mice. Bosutinib, at 150 mg/kg once daily for 5 days a week, is effective against both wild-type Bcr-Abl and mutant Ba/F3 xenografts[2].

Bosutinib 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02551718 Acute Leukemia of Ambiguous Li... 展开 >>neage Recurrent Adult Acute Lymphoblastic Leukemia Recurrent Adult Acute Myeloid Leukemia Recurrent Childhood Acute Lymphoblastic Leukemia Recurrent Childhood Acute Myeloid Leukemia Refractory Acute Myeloid Leukemia Refractory Adult Acute Lymphoblastic Leukemia Refractory Childhood Acute Lymphoblastic Leukemia 收起 << Not Applicable Recruiting - United States, Washington ... 展开 >> Fred Hutch/University of Washington Cancer Consortium Recruiting Seattle, Washington, United States, 98109 Contact: Pamela S. Becker    206-616-1589    pbecker@u.washington.edu    Principal Investigator: Pamela S. Becker 收起 <<
NCT03610971 Chronic Phase Chronic Myeloid ... 展开 >>Leukemia Chronic Myeloid Leukemia, Chronic Phase 收起 << Phase 2 Not yet recruiting January 2022 United States, Florida ... 展开 >> H. Lee Moffitt Cancer Center and Research Institute Not yet recruiting Tampa, Florida, United States, 33612 Contact: Anthony McLaughlin    813-745-5941    anthony.mclaughlin@moffitt.org    Contact: Kendra Sweet, M.D.    813-745-8986    kendra.sweet@moffitt.org    Principal Investigator: Kendra Sweet, M.D. 收起 <<
NCT03746054 Chronic Myeloid Leukemia (CML) Phase 3 Not yet recruiting March 2023 -

Bosutinib 参考文献

[1]Jorge E Cortes, et al. Bosutinib versus imatinib in newly diagnosed chronic-phase chronic myeloid leukemia: results from the BELA trial. J Clin Oncol. 2012 Oct 1;30(28):3486-92.

[2]Miriam Puttini, et al. In vitro and in vivo activity of SKI-606, a novel Src-Abl inhibitor, against imatinib-resistant Bcr-Abl+ neoplastic cells. Cancer Res. 2006 Dec 1;66(23):11314-22.

Bosutinib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.89mL

0.38mL

0.19mL

9.43mL

1.89mL

0.94mL

18.85mL

3.77mL

1.89mL

Bosutinib 技术信息

CAS号380843-75-4
分子式C26H29Cl2N5O3
分子量 530.45
别名 伯舒替尼 (SKI-606) ;SKI-606
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

溶解度

DMSO: 45 mg/mL(84.83 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方

IP 2% DMSO+2% Tween80+30% PEG300+water 10 mg/mL clear

PO 0.5% CMC-Na 35 mg/mL suspension

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