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/ Src / Bosutinib/博舒替尼

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

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

Bosutinib是一种Src和Abl抑制剂，IC50分别为1.2 nM和1 nM。

Bosutinib/博舒替尼 化学结构 CAS号：380843-75-4
Bosutinib/博舒替尼 化学结构
CAS号：380843-75-4
Bosutinib/博舒替尼 3D分子结构
CAS号：380843-75-4
Bosutinib/博舒替尼 化学结构 CAS号：380843-75-4
Bosutinib/博舒替尼 3D分子结构 CAS号：380843-75-4
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Bosutinib/博舒替尼 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:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
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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

 		VEGFR,PDGFR 99%+
Bosutinib ++++

Src, IC50: 1.2 nM

 		99%
Dasatinib monohydrate ++++

Src, IC50: 0.8 nM

 		98%
Quercetin ✔ PKC,Sirtuin 95%
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/博舒替尼 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/博舒替尼 细胞实验

Cell Line
Concentration Treated Time Description References
BEAS-2B cells 5 or 10 μM 30 min To investigate the inhibitory effect of Bosutinib on Src kinase activity, it was found that pretreatment with Bosutinib significantly inhibited O3-induced EGFR phosphorylation. Environ Health Perspect. 2015 Mar;123(3):231-6.
ParC5 cells 0.1–1.0 μM 30 min Bosutinib inhibited IR-induced apoptosis in ParC5 cells and suppressed phosphorylation of PKC δ at Y64 and Y155. Mol Cancer Ther. 2017 Sep;16(9):1989-1998.
KRAS mutant non-small cell lung cancer cells 0.1, 0.5, 1 μM Bosutinib inhibited migration and invasion in KRAS mutant cells but had no significant effect on KRAS wild-type cells. Mol Cancer. 2014 Jan 24;13:13.
NCI-H1792 cells 0.5, 1 μM Bosutinib-induced inhibition of cell migration and invasion was dependent on ACK1, not SRC. Mol Cancer. 2014 Jan 24;13:13.
Human umbilical vein endothelial cells 0.5 μM 3 h To investigate the effect of Bosutinib on human umbilical vein endothelial cells, results showed that Bosutinib treatment did not affect the phosphorylation of eNOS. Hypertension. 2021 Nov;78(5):1527-1540.
K562DOX cells 1 μM 1 h To evaluate the role of ABCB1 in bosutinib transport, results showed the lowest intracellular level of bosutinib in K562DOX cells J Hematol Oncol. 2015 Jul 7;8:81.
K562S cells 1 μM 1 h To evaluate bosutinib transport in normal cells, results showed high intracellular levels of bosutinib in K562S cells J Hematol Oncol. 2015 Jul 7;8:81.
Human umbilical vein endothelial cells 0.5 μM 3 h To investigate the effect of Bosutinib on eNOS phosphorylation in endothelial cells, results showed that Bosutinib treatment did not affect eNOS phosphorylation. Hypertension. 2021 Nov;78(5):1527-1540.
SYF-Src 0.3 µM 48 h SKI-606 significantly inhibited migration and invasion of SYF-Src cells. Mol Cancer Ther. 2008 May;7(5):1185-94
SYF −/− 1 µM 48 h SKI-606 had minimal effects on migration and invasion of SYF −/− cells. Mol Cancer Ther. 2008 May;7(5):1185-94
MCF-7 1 µM 48 h SKI-606 caused cell aggregation and inhibited cell migration and invasion. Mol Cancer Ther. 2008 May;7(5):1185-94
HMDM cells 0.52 μg/mL (1μM) 15 h Enhances macrophage killing of bacteria, reducing intracellular VRE CFU by ∼0.5 log ACS Infect Dis. 2024 May 10;10(5):1725-1738.
BMDM cells 0.52 μg/mL (1μM) 15 h Enhances macrophage killing of bacteria, reducing intracellular VRE CFU by ∼0.5 log ACS Infect Dis. 2024 May 10;10(5):1725-1738.
MDA-MB-231 1 µM 48 h SKI-606 inhibited cell migration and invasion with an IC50 of 0.1–0.3 µM. Mol Cancer Ther. 2008 May;7(5):1185-94
THP-1 cells 0.52 μg/mL (1μM) 15 h Enhances macrophage killing of bacteria, reducing intracellular VRE CFU by ∼0.5 log ACS Infect Dis. 2024 May 10;10(5):1725-1738.
RAW264.7 cells 0.52 μg/mL (1μM) 15 h Enhances macrophage killing of bacteria, reducing intracellular VRE CFU by ∼1 log ACS Infect Dis. 2024 May 10;10(5):1725-1738.
Ba/F3 BCR-ABLT315I cells 1 μM 6 h Evaluate the combined effect on the transcriptome of BCR-ABLT315I cells, showing 645 genes significantly upregulated and 584 genes significantly downregulated Nat Chem Biol. 2012 Nov;8(11):905-912.
Py-230 cells 1 μM 4 days SKI-606 inhibited Py-230 cell proliferation without significant cytotoxic effects Oncogene. 2011 Jan 20;30(3):301-12
MDA-MB-435s 1 µM 48 h SKI-606 caused cell aggregation and inhibited cell migration and invasion. Mol Cancer Ther. 2008 May;7(5):1185-94
MDA-MB-468 1 µM 48 h SKI-606 caused cell aggregation, forming dense clusters, and inhibited cell migration and invasion. Mol Cancer Ther. 2008 May;7(5):1185-94
Non-small cell lung cancer cell lines (KRAS wild type) 0.1, 0.5 and 1 μM 6 h (migration) and 24 h (invasion) No significant effect on migration and invasion of KRAS wild type cells Mol Cancer. 2014 Jan 24;13:13.
Non-small cell lung cancer cell lines (KRAS mutant) 0.1, 0.5 and 1 μM 6 h (migration) and 24 h (invasion) Inhibited migration and invasion of KRAS mutant cells without affecting cell viability Mol Cancer. 2014 Jan 24;13:13.

Bosutinib/博舒替尼 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice KRT5Cre/tdTomatoLoxP transgenic mice Tail vein injection 30 mg/kg Single injection, observed for 3 hours To study the effect of SKI606 on the retraction of basal cell axiopodia, results showed that SKI606 induced the retraction of axiopodia. Nat Commun. 2016 Feb 12;7:10666
Mice Endothelial cell-specific c-Abl knockout mice Oral 100 mg/kg Once daily for 4 to 7 days To investigate the effect of Bosutinib on blood pressure, results showed that Bosutinib treatment increased blood pressure in mice, and this effect was independent of endothelial c-Abl. Hypertension. 2021 Nov;78(5):1527-1540.
Nude mice K562S, K562DOX, and K562DOX/sh P-GP xenograft model Oral 150 mg/kg Once daily, 5 days/week for 2 weeks To evaluate the effect of ABCB1 overexpression on the anti-tumor activity of bosutinib, results showed that K562DOX mice had a limited response to bosutinib treatment and relapsed, while K562DOX/sh P-GP mice were fully sensitive to treatment J Hematol Oncol. 2015 Jul 7;8:81.
Mice Endothelial cell-specific c-Abl knockout mice Oral gavage 100 mg/kg Once daily for 4 to 7 days To investigate the effect of Bosutinib on blood pressure and its mechanism, results showed that Bosutinib increased blood pressure by upregulating soluble epoxide hydrolase (sEH), and the sEH inhibitor TPPU reversed this effect. Hypertension. 2021 Nov;78(5):1527-1540.
Mice Wound infection model Intraperitoneal injection 5 mg/kg Single dose Reduces bacterial load in wounds, decreasing VRE and MRSA CFU by 0.6 log and 1.2 log, respectively ACS Infect Dis. 2024 May 10;10(5):1725-1738.
Mice MMTV-PyMT transgenic mice Oral gavage 150 mg/kg Five consecutive daily treatments followed by two days without treatment for up to 45 additional days SKI-606 significantly suppressed tumor formation, with half of the animals not developing obvious tumors, and induced differentiation of mammary tumors Oncogene. 2011 Jan 20;30(3):301-12
Male Sprague-Dawley rats Polytrauma transfusion model Intravenous injection 5 mg/kg Repeated dose 5 hours after trauma Bosutinib as an adjunct therapy to a balanced transfusion strategy reduced resuscitation volume, improved shock reversal, and reduced vascular leak and organ injury in a rat polytrauma model. Br J Anaesth. 2021 May;126(5):958-966

Bosutinib/博舒替尼 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/博舒替尼 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/博舒替尼 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/博舒替尼 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/博舒替尼 技术信息

CAS号380843-75-4
分子式C26H29Cl2N5O3
分子量 530.45
SMILES Code N#CC1=C(NC2=CC(OC)=C(Cl)C=C2Cl)C3=CC(OC)=C(OCCCN4CCN(C)CC4)C=C3N=C1
MDL No. MFCD07367846
别名 伯舒替尼 (SKI-606) ;SKI-606
运输蓝冰
InChI Key UBPYILGKFZZVDX-UHFFFAOYSA-N
Pubchem ID 5328940
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一
方案 二
方案 三

Tags: Bosutinib | SKI-606 | 伯舒替尼 (SKI-606) | Src | AmBeed-信号通路专用抑制剂 | Bosutinib/博舒替尼 纯度/质量文件 | Bosutinib/博舒替尼 亚型比较 | Bosutinib/博舒替尼 生物活性 | Bosutinib/博舒替尼 临床数据 | Bosutinib/博舒替尼 参考文献 | Bosutinib/博舒替尼 实验方案 | Bosutinib/博舒替尼 技术信息

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