Bosutinib

SKU: orb1225150

Description

Bosutinib is a Bcr-Abl kinase inhibitor for the treatment of Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML). Compared to other tyrosine kinase inhibitors, it has a more favourable hematologic toxicity profile. FDA approved on September 4, 2012. (In Vitro):Bosutinib (SKI-606) is an active inhibitor of Bcr-Abl in several chronic myelogenous leukemia cell lines, with IC50 values in the low nanomolar range.(In Vivo):Bosutinib (oral gavage; 75 mg/kg twice daily or 150 mg/kg once daily) has activity against human KU812 xenografts in nude mice. Bosutinib (150 mg/kg; once daily, 5 days weekly) has activity against syngeneic Bcr-Abl WT and mutant Ba/F3 xenografts.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 380843-75-4
• MW: 530.45
• Purity: >98% (HPLC)
• Formula: C₂₆H₂₉Cl₂N₅O₃
• SMILES: N#CC1=C(NC2=CC(OC)=C(Cl)C=C2Cl)C3=CC(OC)=C(OCCCN4CCN(C)CC4)C=C3N=C1
• Target: Bcr-Abl
• Solubility: Ethanol: 2 mg/mL (3.77 mM); DMSO: 100 mg/mL (188.51 mM)

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SKI 606

Quick Database Links

Gene Symbol

Bcr-Abl