Pulrodemstat HCl

SKU: orb2695157

Description

Pulrodemstat HCl is a potent, selective, and orally bioavailable inhibitor of lysine-specific demethylase 1 (LSD1/KDM1A). It demonstrates anti-proliferative and pro-apoptotic activity in head and neck squamous cell carcinoma (HNSCC) models, inhibiting cell proliferation and migration in vitro and tumor growth in vivo.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1821307-11-2
• MW: 487.93
• Purity: 99.16%
• Formula: C₂₄H₂₄ClF₂N₅O₂
• SMILES: Cl.N#CC1=CC=C(C=C1F)C=2N=C(N(C(=O)C2C=3C=CC(OC)=C(F)C3)C)N4CCC(N)CC4
• Target: Histone Demethylase

Bioactivity

• Target IC50:
  H1417 cells:4 nM (EC50)|CD11b:7 nM (EC50)|H209 cells:3 nM (EC50)
• In Vivo:
  In a patient-derived xenograft SCLC model, daily oral administration of 5 mg/kg Pulrodemstat HCl for 30 days significantly inhibited tumor growth. In addition, in a SCLC xenograft mouse model (H1417), once-daily treatment with Pulrodemstat HCl for 4 consecutive days significantly down-regulated GRP mRNA levels at 2.5 mg/kg, while the strongest inhibition of GRP expression was observed at 5 mg/kg. After intravenous injection of 5 mg/kg Pulrodemstat HCl, the systemic clearance was 32.4 mL/min/kg, the elimination half-life was 2 h, and the volume of distribution was high at 7.5 L/kg. When the same dose was administered orally, the drug was well absorbed, with an AUC (0-24h) of 1.8 μM-h, Cmax of 0.36 μM, oral bioavailability of 0.36 μM, and oral bioavailability of 1.8 μM/kg. μM and oral bioavailability was 32%.
• In Vitro:
  Pulrodemstat HCl was effective in inducing the target cell differentiation marker CD11b in the THP-1 cell line with an EC50 of 7 nM; the antiproliferative activity in AML Kasumi-1 cells had an EC50 of 2 nM. Pulrodemstat HCl acts for 4 days and inhibits GRP in a dose-dependent manner at pharmacologically useful concentrations (H209-EC50=3 nM and H1417-EC50=4 nM).Pulrodemstat HCl acts for 12 days and produces potent antiproliferative activity (H1417-EC50=6 nM) in SCLC cells.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Pulrodemstat HCl(1821307-10-1 Free base), CC90011 HCl, CC-90011 HCl, LSD1-IN-7 HCl

Compound Identifiers

PubChem CID

129096973