Bosutinib

SKU: orb1310890

Description

Bosutinib

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 380843-75-4
• MW: 530.45
• Purity: 99.89%
• Formula: C₂₆H₂₉Cl₂N₅O₃
• SMILES: N(C=1C2=C(C=C(OCCCN3CCN(C)CC3)C(OC)=C2)N=CC1C#N)C4=CC(OC)=C(Cl)C=C4Cl
• Target: Autophagy,Src,Bcr-Abl
• Solubility: DMSO:65 mg/mL (122.54 mM);Ethanol:13.3 mg/mL (25.07 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.77 mM)

Bioactivity

• Target IC50:
  Abl:1 nM (cell free)|Src:1.2 nM (cell free)
• In Vivo:
  Bosutinib (30/25 mg/kg, b.i.d) reduces tumor growth in unstaged and staged Src-transformed fibroblast mouse xenograft models. Bosutinib (100 mg/kg) also induces complete tumor regression in a K562 mouse xenograft model when administered once per day for five days.
• In Vitro:
  Bosutinib ha the ant Proliferative activity against three different Bcr-Abl-positive leukemia cell lines (KU812, K562, and MEG-01). Bosutinib inhibite the proliferation of All three cell lines, with IC50 ranging from 5 nM in the KU812 line to 20 nM fo the K562 and MEG-01 cell lines. Inhibition of proliferation by Bosutinib is associated with cell cycle arrest and cell death. Treatment with Bosutinib at 100 nM for 24 h (KU812) or 48 h (K562) resulted in a reduction of S and G2-M phase cells and an increase of cells with a DNA content of less than 2N. Treatment with Bosutinib at 100 nM also led to PARP degradation after 48 h the potent ant Proliferative activity of Bosutinib against mL lines was not a general property for leukemia cell lines. Molt-4, HL-60, Ramos, and Other leukemia cell lines were unaffected by Bosutinib at concentration less than 1 μM.
• Cell Research:
  Cells are exposed to various concentration of Bosutinib for 72 hours. Anchorage-independent proliferation of Abl-MLV-transformed fibroblasts is measured in 96-well ultra-low binding plates treated with Sigmacote to block residual cell attachment. Cell proliferation is measured with MTS or Cell-Glo. Fo the determination of cell cycle or cell death, cells are prepared for FACS analysis in the CycleTest Plus DNA reagent kit and analyzed on a fluorescence-activated cell sorter flow cytometer.
• Animal Research:
  K562 cells were suspended to 50 million cells mL in Matrigel (1 volume of cells with 1 volume of cold Matrigel). Nude f Male mice 6–7 weeks of age were given injections of 0.2 ml of this suspension. Tumors were staged for 10 days, at which time they entere the growth phase. At this time the compound was administered by oral gavage in a 0.2 ml suspension with 0.5% methocel/0.4% Tween 80.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Src, Src/Abl tyrosine kinase inhibitor, SKI606, SKI-606, SKI 606, Inhibitor, Oral, inhibit, Abl, cancer, Bosutinib, Bcr-Abl, BcrAbl, Autophagy, c-Src

Compound Identifiers

PubChem CID

5328940