380843-81-2
Chemical Structure
N-Desmethyl-Bosutinib
Synonym(s): N-Desmethyl-SKI-606
- CAS No.: 380843-81-2
- Formula:C25H27Cl2N5O3
- Molecular Weight:516.42
IUPAC Name: 4-((2,4-dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(piperazin-1-yl)propoxy)quinoline-3-carbonitrile
InChIKey: WJNXCARNBUNEMQ-UHFFFAOYSA-N
SMILES: N#CC1=C(NC2=CC(OC)=C(Cl)C=C2Cl)C3=CC(OC)=C(OCCCN4CCNCC4)C=C3N=C1
Biological Activity: N-Desmethyl-Bosutinib (N-Desmethyl-SKI-606) is the N-demethylated metabolite of Bosutinib (HY-10158), and also acts as a Src kinase inhibitor with an IC50 of 1.1 nM. N-Desmethyl-Bosutinib inhibits the enzymatic activity of Src kinase as well as Src-dependent cell proliferation, and can be used in the research of chronic myeloid leukemia[1][2][3][4][5].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
N-Desmethyl-Bosutinib | N-Desmethyl-Bosutinib (N-Desmethyl-SKI-606) is the N-demethylated metabolite of Bosutinib (HY-10158), and also acts as a Src kinase inhibitor with an IC50 of 1.1 nM. N-Desmethyl-Bosutinib inhibits the enzymatic activity of Src kinase as well as Src-dependent cell proliferation, and can be used in the research of chronic myeloid leukemia. | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [1]. Boschelli DH, et al. Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity. Journal of medicinal chemistry. 2001 Nov 08;44(23):3965-77. [Content Brief]
- [2]. Adiwidjaja J, et al. Physiologically-Based Pharmacokinetic Predictions of the Effect of Curcumin on Metabolism of Imatinib and Bosutinib: In Vitro and In Vivo Disconnect. Pharmaceutical research. 2020 Jun 11;37(7):128.
- [3]. Adiwidjaja J, et al. Physiologically based pharmacokinetic model predictions of natural product-drug interactions between goldenseal, berberine, imatinib and bosutinib. European journal of clinical pharmacology. 2022 Apr;78(4):597-611.
- [4]. Adiwidjaja J, et al. Potential for pharmacokinetic interactions between Schisandra sphenanthera and bosutinib, but not imatinib: in vitro metabolism study combined with a physiologically-based pharmacokinetic modelling approach. British journal of clinical pharmacology. 2020 Oct;86(10):2080-2094.
- [5]. Abbas R, et al. Evaluation of the pharmacokinetics and safety of bosutinib in patients with chronic hepatic impairment and matched healthy subjects. Cancer chemotherapy and pharmacology. 2013 Jan;71(1):123-32.
