PD180970

SKU: orb1704251

Description

PD180970 is a potent small molecule inhibitor targeting Bcr-Abl, Src, and Kit kinases, with respective IC50 values of 5 nM, 0.8 nM, and 50 nM. It is a valuable research tool for in vitro and in vivo studies investigating the mechanisms and treatment of chronic myelogenous leukemia and related tyrosine kinase-driven pathologies.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 287204-45-9
• MW: 429.27
• Purity: 98.67% (May vary between batches)
• Formula: C₂₁H₁₅Cl₂FN₄O
• SMILES: Cc1cc(Nc2ncc3cc(-c4c(Cl)cccc4Cl)c(=O)n(C)c3n2)ccc1F
• Target: Bcr-Abl,Src,c-Kit,Apoptosis
• Solubility: 10% DMSO+90% Corn Oil:1 mg/mL (2.33 mM);DMSO:90 mg/mL (209.66 mM)

Bioactivity

• Target IC50:
  c-Kit:50 nM|Src:0.8 nM|BCR-ABL:5 nM (Ip210Bcr-Ablkinase)
• In Vivo:
  In Male C57BL/6J mice injected with MPTP, intraperitonial injection of PD180970 (5 mg/kg) decreased number of activated microglia on activation by MPTP and reduces the Iba1 expression intensity in activated microglia.
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• In Vitro:
  In K562 cells, PD180970 (0.5 μM) induces apoptosis and causes cell death. The IC50 values are 170, 80, and 80 nM for the tyrosine phosphorylation of p210Bcr-Abl, Gab2, and CrkL. PD180970 significantly inhibits the purified recombinant Abl tyrosine kinase activity with an IC50 of 2.2 nM. In the human K562 CML cells, PD180970 inhibits the activity of Stat5 DNA-binding with an IC50 of 5 nM.
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Storage & Handling

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

Alternative Names

cKit, BcrAbl, Bcr-Abl, Kit, PD 180970, PD180970, PD-180970, Src

Compound Identifiers

PubChem CID

5311104