PD-173955

SKU: orb1222448

Description

PD-173955 is a src tyrosine kinase inhibitor. PD173955 inhibited Bcr-Abl-dependent cell growth. PD173955 showed cell cycle arrest in G(1). PD173955 has an IC(50) of 1-2 nM in kinase inhibition assays of Bcr-Abl, and in cellular growth assays it inhibits Bcr-Abl-dependent substrate tyrosine phosphorylation. PD173955 inhibited kit ligand-dependent c-kit autophosphorylation (IC(50) = approximately 25 nM) and kit ligand-dependent proliferation of M07e cells (IC(50) = 40 nM) but had a lesser effect on interleukin 3-dependent (IC(50) = 250 nM) or granulocyte macrophage colony-stimulating factor (IC(50) = 1 microM)-dependent cell growth.

Key Properties

• CAS Number: 260415-63-2
• MW: 443.35
• Purity: >98% (HPLC)
• Formula: C₂₁H₁₆Cl₂N₄OS
• SMILES: CSc1cccc(Nc2ncc3cc(c(=O)n(C)c3n2)c2c(Cl)cccc2Cl)c1
• Target: Antioxidant
• Solubility: DMSO : ≥ 32 mg/mL; 72.18 mM

Bioactivity

• In Vivo:
  Animal model: Balb/c mice model of chronic myeloid leukemia (CML). Dosage: 50 mg/kg. Administration: Oral gavage (p.o.), Twice daily for 4 days. Result: Significantly inhibited constitutive tyrosine phosphorylation of numerous proteins (including Lyn) in primary Bcr/abl expressing leukemia cells. Reduced the number of mice with splenomegaly and inhibited splenomegaly in at least half of the mice compared to the control group. Was effective in reducing the peripheral blood granulocytosis of the murine CML-like disease.
• In Vitro:
  Cell Cycle Analysis Cell line: MDA-MB-468. Concentration: 5 μM. Incubation time: 24 h. Result: Blocked 95% of the cells in the G2-M phase. Cell Proliferation Assay Cell line: MO7e, R10(-)(a cell line derived from P210-MO7e). Concentration: 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM Incubation time: 48 h. Result: Completely blocked the growth of R10 cells at 2.5 nM. Inhibited stem cell factor (SCF) -dependent proliferation at 5-10 nM and completely inhibited SCF-dependent growth at 50 nM.

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

PD173955 | PD 173955

Quick Database Links

Gene Symbol

Antioxidant