PD180970

SKU: orb2901466

Description

PD180970 is a highly potent and ATP-competitive p210Bcr-Abl kinase inhibitor, with an IC50 of 5 nM for inhibiting the autophosphorylation of p210Bcr-Abl. PD180970 also inhibits Src and KIT kinase with IC50s of 0.8 nM and 50 nM, respectively. PD180970 indcues apoptosis of K562 leukemic cells, and can be used for chronic myelogenous leukemia research.

Key Properties

• CAS Number: 287204-45-9
• MW: 429.27
• Purity: >98% (HPLC)
• Formula: C₂₁H₁₅Cl₂FN₄O
• SMILES: Cc1cc(Nc2ncc3cc(-c4c(Cl)cccc4Cl)c(=O)n(C)c3n2)ccc1F
• Target: Bcr-Abl
• Solubility: In Vitro: DMSO : 100 mg/mL (232.95 mM; Ultrasonic )

Bioactivity

• In Vivo:
  PD180970 (5 mg/kg; intraperitonial injection; daily; for 7 days) mitigates MPTP-induced neuronal loss in mice. PD180970 has the neuroprotective ability in a preclinical mouse model of Parkinson's disease (PD). Animal model: Male C57BL/6J mice (3-4 months old) injected with MPTP. Dosage: 5 mg/kg. Administration: Intraperitonial injection; daily; for 7 days. Result: Decreased number of activated microglia on activation by MPTP in mice brains. And showed significant reduction in intensity of Iba1 expression in activated microglia.
• In Vitro:
  PD180970 (0.5 μM; 24-96 hours) treatment causes cell death K562 cells. PD180970 (0.5 μM; 24-48 hours) treatment induces apoptosis of K562 cells. The result shows increase in annexin V-PI double-positive cells. PD180970 inhibits tyrosine phosphorylation of p210Bcr-Abl, Gab2, and CrkL in K562 cells with IC50 values of 170 nM, 80 nM, and 80 nM, respectively. In vitro, PD180970 potently inhibits autophosphorylation of p210Bcr-Abl (IC50 of 5 nM) and the kinase activity of purified recombinant Abl tyrosine kinase (IC50 of 2.2 nM). The blocking Bcr-Abl kinase activity using PD180970 in the human K562 CML cell line resulted in inhibition of Stat5 DNA-binding activity with an IC50 of 5 nM. Cell Viability Assay Cell line: K562 cells. Concentration: 0.5 μM Incubation time: 24 hours, 48 hours, 72 hours, 96 hours. Result: Resulted in cell death. Apoptosis Analysis Cell line: K562 cells. Concentration: 0.5 μM Incubation time: 24 hours, 48 hours. Result: Increased annexin V-positive/PI-negative cells.

Storage & Handling

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

Quick Database Links

Gene Symbol

Bcr-Abl