KA2507

SKU: orb1218682

Description

KA2507 is a potent and selective HDAC6 inibitor with an IC50 of 2.5nM.

Key Properties

• CAS Number: 1636894-46-6
• MW: 322.32
• Purity: >98% (HPLC)
• Formula: C₁₆H₁₄N₆O₂
• SMILES: O=C(NO)C1=CC=C(CN(C2=NC=CN=C2)C3=NC=CN=C3)C=C1
• Target: HDAC
• Solubility: DMSO : 60 mg/mL (186.15 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  KA2507 (100-200 mg/kg; p.o. ; daily; for 20 days) inhibits tumor growth in the syngeneic B16-F10 mouse melanoma model. KA2507 also demonstrates antitumor efficacy in CT26 and MC38 colorectal cancer models. Analysis of tumor samples also indicates modulation of biomarkers of antitumor immunity at efficacious dosing, with KA2507 administration resulting in reduced STAT3 activation (as measured by phospho-STAT3, an important suppressor of the antitumor immune response), reduced PD-L1 expression, and increased expression of MHC class I. KA2507 exhibits poor oral bioavailability (mice 15%) and Cmax (mice 300 ng/mL) following oral administration (mice 200 mg/kg). Animal model: Male C57BL/6 mice, B16-F10 melanoma model. Dosage: 100 mg/kg, 200 mg/kg, 200 mg/kg. Administration: Oral gavage, daily, for 20 days. Result: Demonstrated antitumor efficacy. Animal model: Male C57BL/6 mice. Dosage: 200 mg/kg (Pharmacokinetic Analysis). Administration: Oral administration. Result: Oral bioavailability (15%), Cmax (300 ng/mL).
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• In Vitro:
  KA2507 did not inhibit the in vitro proliferation of mouse or human cancer cells at concentrations that are selective for HDAC6 inhibition.

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

HDAC