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  A820    
Bosutinib
, 98% (HPLC)
 
4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-3-quinolinecarbonitrile




IDENTITY
CAS Number:380843-75-4
MDL Number:MFCD07367846
MF:C26H29Cl2N5O3
MW:530.45
SPECIFICATIONS & PROPERTIES
Min. Purity Spec:98% (HPLC)
Physical Form (at 20°C):Solid
Melting Point:137-147°C
Density:1.36
Long-Term Storage:Store long-term in a cool, dry place
DOT/IATA TRANSPORT INFORMATION
Not hazardous material

BIOLOGICAL INFO
Solubility:DMSO: >=15mg/mL
Application(s):Dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM

REVIEW

 Dual inhibitor of Abl and Src kinases (IC50 = 1.2 nM for Src in an enzymatic assay). Displays antiproliferative activity against chronic myelogenous leukemia (CML) cells and decreases the motility and invasion of breast cancer cell lines. Also exhibits potent antiproliferative activity in anchorage-independent, Src-transformed rat fibroblasts (IC50 = 100 nM). Displays selectivity for Src over non-Src family kinases such as growth factor receptor tyrosine kinases.

REFERENCES
[1]Cortes JE, Kantarjian HM, Brümmendorf TH, Kim DW, Turkina AG, Shen ZX, Pasquini R, Khoury HJ, Arkin S, Volkert A, Besson N, Abbas R, Wang J, Leip E, Gambacorti-Passerini C. Safety and efficacy of bosutinib (SKI-606) in chronic phase Philadelphia chromosome-positive chronic myeloid leukemia patients with resistance or intolerance to imatinib. Blood. 2011 Oct 27;118(17):4567-76. Epub 2011 Aug 24.
[2] Cortes JE, Kim DW, Kantarjian HM, Brümmendorf TH, Dyagil I, Griskevicus L, Malhotra H, Powell C, Gogat K, Countouriotis AM, Gambacorti-Passerini C. Bosutinib Versus Imatinib in Newly Diagnosed Chronic-Phase Chronic Myeloid Leukemia: Results From the BELA Trial. J Clin Oncol. 2012 Sep 4. [Epub ahead of print]
[3] Bosulif Approved for Previously Treated Philadelphia Chromosome-Positive Chronic Myelogenous Leukemia.
[4] Boschelli et al (2001) Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity. J.Med.Chem. 44 3965. PMID: 11689083.

GLOBALLY HARMONIZED SYSTEM (GHS)

Pictograms

Signal Word
Warning

Hazard Statements
H319; H413

Precautionary Statements
P264; P273; P280; P305+P351+P338; P337+P313; P501


RELATED PRODUCTS
A820Bosutinib
X48404-(3,5-Dichloro-4-methoxyanilino)-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinoline-3-carbonitrile

Current as of November 17, 2024


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All products are stocked and shipped from the SF Bay, California, USA via FedEx, UPS or DHL.
All batches backed with full quality assurance.
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All products are for research and development use only, not for any other uses, and must be handled by technically-qualified persons.

These products are explicitly not intended to be used in foods and/or cosmetics and/or drugs (human and veterinary) and/or consumer products and/or biocides and/or pesticides of any kind unless explicitly stated otherwise.

Products are not sold to individuals. We do not ship to residential addresses. Consumer orders will be cancelled without notice.

New customers undergo an internal onboarding process. As part of this process, new customers may be asked for more information. Additional restrictions may apply.



CATEGORIES

 APIs and Bioactives > Protein Kinase Inhibitors


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