KA2507

SKU: orb1298330

Description

KA2507 is a highly selective HDAC6 inhibitor exhibiting potent activity with an IC50 of 2.5 nM. This research compound is used in vitro and in vivo to study HDAC6's role in oncology, neurology, and immunology.

Research Area

Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 1636894-46-6
• MW: 322.32
• Purity: 99.14% (May vary between batches)
• Formula: C₁₆H₁₄N₆O₂
• SMILES: ONC(=O)c1ccc(CN(c2cnccn2)c2cnccn2)cc1
• Target: HDAC
• Solubility: DMSO:60 mg/mL (186.15 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.21 mM)

Bioactivity

• Target IC50:
  HDAC8:621|HDAC6:2.5nm
• In Vivo:
  KA2507 (100-200 mg/kg; p.o.; daily; for 20 days) inhibits tumor growth in the syngeneic B16-F10 mouse melanoma model and shows antitumor efficacy in CT26 and MC38 colorectal cancer models. Tumor sample analysis reveals that at efficacious doses, KA2507 modulates biomarkers of antitumor immunity, resulting in reduced STAT3 activation (measured by phospho-STAT3), decreased PD-L1 expression, and increased MHC class I expression. However, KA2507 exhibits poor oral bioavailability (mice 15%) and Cmax (mice 300 ng/mL) following oral administration (mice 200 mg/kg).
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• In Vitro:
  At concentrations selective for HDAC6 inhibition, KA2507 did not inhibit in vitro proliferation of mouse or human cancer cells.

Storage & Handling

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

Alternative Names

antitumor, cancer, colorectal, modulatory, immune, inhibit, KA 2507, KA2507, KA-2507, HDAC8, HDAC, HDAC6, Inhibitor, melanoma, Histone deacetylases

Compound Identifiers

PubChem CID

117703516