ChemicalBook > CAS DataBase List > Bosutinib Monohydrate

Bosutinib Monohydrate

Product Name: Bosutinib Monohydrate
CAS No.: 918639-08-4
Chemical Name: Bosutinib Monohydrate
Synonyms: bosutinib hydrate;Bosutinib Monohydrate;Bosutinib MonohydrateQ: What is Bosutinib Monohydrate Q: What is the CAS Number of Bosutinib Monohydrate;4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile hydrate
CBNumber: CB62728577
Molecular Formula: C26H31Cl2N5O4
Formula Weight: 548.47
MOL File: 918639-08-4.mol

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Bosutinib Monohydrate Property

form: Solid
color: White to off-white
InChIKey: BXPOSPOKHGNMEP-UHFFFAOYSA-N
SMILES: N(C1C(=CC(Cl)=C(OC)C=1)Cl)C1=C(C=NC2C=C(OCCCN3CCN(C)CC3)C(OC)=CC1=2)C#N.O

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H317May cause an allergic skin reaction

H400Very toxic to aquatic life

H410Very toxic to aquatic life with long lasting effects

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P272Contaminated work clothing should not be allowed out of the workplace.

P273Avoid release to the environment.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P321Specific treatment (see … on this label).

P333+P313IF SKIN irritation or rash occurs: Get medical advice/attention.

P363Wash contaminated clothing before reuse.

P391Collect spillage. Hazardous to the aquatic environment

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Biosynth Carbosynth

Product number: FB145112
Product name: Bosutinib monohydrate
Packaging: 100mg
Price: $120
Updated: 2021/12/16

Biosynth Carbosynth

Product number: FB145112
Product name: Bosutinib monohydrate
Packaging: 250mg
Price: $200
Updated: 2021/12/16

Biosynth Carbosynth

Product number: FB145112
Product name: Bosutinib monohydrate
Packaging: 1g
Price: $400
Updated: 2021/12/16

AK Scientific

Product number: 4958BB
Product name: Bosutinibmonohydrate
Packaging: 500mg
Price: $455
Updated: 2021/12/16

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Bosutinib Monohydrate Chemical Properties,Usage,Production

Uses

Bosutinib hydrate is an oraly activel Src/Abl tyrosine kinase inhibito with IC50 of 1.2 nM and 1 nM, respectively[1].

Definition

ChEBI: A hydrate that is the monohydrate form of anhydrous bosutinib.

Clinical Use

Bosulif ® (Bosutinib hydrate), also known as (SKI-606), is a novel 4-phenylamino-3-quinolinecarbonitrile kinase inhibitor approved for treatment of adults with chronic, accelerated, or blast phase Philadelphia chromosome-positive chronic myeloid leukemia (Ph+CML). Bosutinib is an orally-dosed, dual Src/Abl kinase inhibitor which provides an alternative treatment to patients exhibiting immunity to imatinib and other kinase inhibitors utilized for this treatment. In contrast to competitor tyrosine inhibitors, bosutinib inhibits autophosphorylation of both Srs and Abl kinases, leading to decreased cell growth and apoptosis. Bosutinib was originally developed by Wyeth and continues to be marketed by Pfizer after the merger of Wyeth and Pfizer in 2009.

Synthesis

Several synthetic routes to bosutinib have been reported, including synthetic work for scale up and processing to obtain pure salt forms of bosutinib for pharmaceutical applications.56-59 The current manufacturing route begins with reaction of 2-methoxy-5-nitrophenol (36) and 1-bromo-3- chloropropane (37) to provide aryl chloroether 38 in 82% yield. Reaction of 38 with Nmethylpiperazine (39) and NaI in refluxing DME provided the functionalized aryl-nitro-piperazine 40 (77% yield), which was converted directly to aniline 41 under hydrogenolysis conditions. Aniline 41 was then reacted with triethyl orthoformate and aryl cyanoamide 42, which was generated in one step from 2,4-dichloro-5-methoxy-aniline (44), 1,3-diisopropylcabodiimide (DIC), and cyanoacetic acid (45) under refluxing conditions, to yield advanced intermediate 43 (93% over 2 steps). Finally, conversion of 43 to bosutinib was facilitated by a POCl3-promoted cyclization in the presence of sulfolane. As shown in Scheme 8, employment of carefully optimized conditions for the isolation of bosutinib hydrate (VII) provided material in 75-82% yields and >99% purity.

in vivo

Bosutinib (oral gavage; 75 mg/kg twice daily or 150 mg/kg once daily) hydrate has activity against human KU812 xenografts in nude mice. Bosutinib (150 mg/kg; once daily, 5 days weekly) hydrate has activity against syngeneic Bcr-Abl WT and mutant Ba/F3 xenografts^[2].

Animal Model:	KU812CM L xenograft model^[2]
Dosage:	75 mg/kg twice daily or 150 mg/kg once daily
Administration:	Bosutinib (oral gavage; 75 mg/kg twice daily or 150 mg/kg once daily)
Result:	Had the therapeutic activity and produced a dose- and schedule-dependent weight loss.

Animal Model:	Syngeneic Bcr-Abl WT and mutant Ba/F3 xenografts^[2]
Dosage:	150 mg/kg
Administration:	Bosutinib (150 mg/kg; once daily, 5 days weekly)
Result:	Decreased the rate of tumor growth and prolonged event-free survival of mice.

References

[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. DOI:10.1200/JCO.2011.38.7522
[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. DOI:10.1158/0008-5472.CAN-06-1199

Bosutinib Monohydrate Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Bosutinib Monohydrate manufacturers

Career Henan Chemical Co

Product: Bosutinib Monohydrate 918639-08-4
Price: US $2.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: ask
Release date: 2018-12-23

918639-08-4, Bosutinib MonohydrateRelated Search:

5-Amino-2,4-dichloroanisole 2-aMino-4-(3-chloropropoxy)-5-Methoxybenzoate 4-CHLORO-7-(3-CHLORO-PROPOXY)-6-METHOXY-QUINOLINE-3-CARBONITRILE Methyl 4-(3-chloropropoxy)-5-Methoxy-2-nitrobenzoate 7-(3-CHLORO-PROPOXY)-4-(2,4-DICHLORO-5-METHOXY-PHENYLAMINO)-6-METHOXY-QUINOLINE-3-CARBONITRILE Bosutinib 4-[(2,4-Dichloro-5-methoxyphenyl)amino]-7-fluoro-6-methoxy-3-quinolinecarbonitrile 3-Quinolinecarbonitrile, 7-(3-chloropropoxy)-4-hydroxy-6-Methoxy- 1-[3-(2-Methoxy-5-nitrophenoxy)propyl]-4-Methylpiperazine N-(2,4-DICHLORO-5-HYDROXYPHENYL)ACETAMIDE 4-Methoxy-3-(3-(4-Methylpiperazin-1-yl)propoxy)aniline 4-CHLORO-7-FLUORO-6-METHOXY-QUINOLINE-3-CARBONITRILE 4-CHLORO-7-HYDROXY-6-METHOXY-QUINOLINE-3-CARBONITRILE 2-CYANO-N-(2,4-DICHLORO-5-METHOXYPHENYL) ACETAMIDE

Bosutinib Monohydrate

bosutinib hydrate

Bosutinib MonohydrateQ: What is Bosutinib Monohydrate Q: What is the CAS Number of Bosutinib Monohydrate

4-((2,4-Dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile hydrate

918639-08-4

C26H31Cl2N5O4

C26H29Cl2N5O3H2O