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Cat. No.: HY-107449

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N-Desmethyl-Bosutinib

Name: N-Desmethyl-Bosutinib
Brand: MedChemExpress
SKU: HY-107449
Availability: PreOrder

(Synonyms: N-Desmethyl-SKI-606)

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.

For research use only. We do not sell to patients.

CAS No.: 380843-81-2
Formula: C₂₅H₂₇Cl₂N₅O₃
Molecular Weight:516.42

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

N-Desmethyl-Bosutinib Chemical Structure

CAS No.: 380843-81-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
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Biological Activity

Description

IC₅₀ & Target

Her3

All Src Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Fibroblast	IC50	1700 nM	Inhibition of anchorage-independent proliferation of c-Src-transformed rat fibroblasts growing in suspension. Inhibition of anchorage-independent proliferation of c-Src-transformed rat fibroblasts growing in suspension.	11689083

In Vitro

N-Desmethyl-Bosutinib (N-Desmethyl-SKI-606) (compound 31e) potently inhibits purified Src kinase with an IC₅₀ of 1.1 nM^[1].
N-Desmethyl-Bosutinib inhibits the anchorage-independent proliferation of c-Src-transformed rat fibroblasts with an IC₅₀ of 1700 nM^[1].
N-Desmethyl-Bosutinib (1-20 μM; 60 min) forms via CYP3A4-mediated N-demethylation of Bosutinib (HY-10158) in human liver microsomes^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Related Protocols :

Chemical Information

CAS No. 380843-81-2
Molecular Weight 516.42
Formula C₂₅H₂₇Cl₂N₅O₃
SMILES

N#CC1=C(NC2=CC(OC)=C(Cl)C=C2Cl)C3=CC(OC)=C(OCCCN4CCNCC4)C=C3N=C1
Synonyms

N-Desmethyl-SKI-606
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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