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PZ0192

Sigma-Aldrich

Bosutinib

≥98% (HPLC)

别名:

4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-3-quinolinecarbonitrile, SKI-606, WAY-173606

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About This Item

经验公式（希尔记法）:
C26H29Cl2N5O3
CAS号:
380843-75-4
分子量:
530.45
MDL编号:
MFCD07367846
UNSPSC代码:
12352200
PubChem化学物质编号:
329823766
NACRES:
NA.77

质量水平

100

方案

≥98% (HPLC)

表单

powder

颜色

off-white to light brown

溶解性

DMSO: ≥15 mg/mL

储存温度

room temp

SMILES字符串

COc1cc(Nc2c(cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)C#N)c(Cl)cc1Cl

InChI

1S/C26H29Cl2N5O3/c1-32-6-8-33(9-7-32)5-4-10-36-25-13-21-18(11-24(25)35-3)26(17(15-29)16-30-21)31-22-14-23(34-2)20(28)12-19(22)27/h11-14,16H,4-10H2,1-3H3,(H,30,31)

InChI key

UBPYILGKFZZVDX-UHFFFAOYSA-N

基因信息

human ... ABL1(25) , HCK(3055) , LYN(4067) , SRC(6714)

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一般描述

Bosutinib is a safe oral medicine with good bioavailability. It is effective for treating chronic myeloid leukemia (CML). It is also a potent ATP-competitive inhibitor for Src tyrosine kinase. Bosutinib inhibits epidermal growth factor receptor (EGFR). It suppresses solid tumors associated with breast, pancreas and prostate.

生化/生理作用

Bosutinib (SKI-606) is an orally active; dual Src/Abl tyrosine kinase inhibitor with potent antiproliferative activity. It does not appear to inhibit c-Kit and PDGRF, which are thought to be the cause of numerous side effects in anticancer treatment with some other tyrosine kinase inhibitors.
Orally active, dual Src/Abl kinase inhibitor with potent antiproliferative activity

特点和优势

This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound is featured on the Abl page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

其他说明

Sigma-Aldrich is a licensed supplier of Bosutinib, providing the authentic Pfizer compound. The material is independently assayed and verified by both Pfizer and Sigma-Aldrich.

法律信息

Sold for research purposes under agreement from Pfizer Inc.

象形图

Exclamation mark
GHS07

警示用语：

Warning

危险声明

H319,H413

预防措施声明

P273 - P305 + P351 + P338

危险分类

Aquatic Chronic 4 - Eye Irrit. 2

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000341977
0000341977
0000296407
0000296407
0000225975

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Jun Imagawa et al.
The Lancet. Haematology, 2(12), e528-e535 (2015-12-22)
First-line imatinib treatment can be successfully discontinued in patients with chronic myeloid leukaemia after deep molecular response has been sustained for at least 2 years. We investigated the safety and efficacy of discontinuing second-line or subsequent dasatinib after at least
Phase I study of bosutinib, a src/abl tyrosine kinase inhibitor, administered to patients with advanced solid tumors.
Daud AI, et al.
Clinical Cancer Research, 18(4), 1092-1100 (2012)
Sawsan M Amer et al.
Chemistry Central journal, 11(1), 136-136 (2017-12-24)
Masitinib (MST) is a selective tyrosine kinase inhibitor. Validated liquid chromatography tandem mass spectrometric method (LC-MS/MS) was developed for the quantification of MST in rat liver microsomes (RLMs) matrix. The developed method was applied to metabolic stability and excretion rate
Takeo Yasu et al.
Biological & pharmaceutical bulletin, 41(2), 254-258 (2017-12-08)
Ponatinib, a novel tyrosine kinase inhibitor marketed in 2016, is a key drug used for treating chronic myeloid leukemia and Philadelphia chromosome-positive acute lymphoblastic leukemia. This study aimed to develop a simple method for determining plasma ponatinib concentration. The analysis
Safety and efficacy of bosutinib (SKI-606) in chronic phase Philadelphia chromosome-positive CML patients with resistance or intolerance to imatinib.
Cortes JE, et al.
Blood, 118(17), 4567-4576 (2011)
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