CCT251236

SKU: orb1707484

Description

CCT251236 is a cell-based phenotypic high-throughput screening probe that inhibits the HSF1 stress pathway. This small molecule demonstrates antimyeloma activity in vitro and has been utilized in oncology research to study heat shock response and protein homeostasis mechanisms.

Research Area

Cell Biology

Key Properties

• CAS Number: 1693731-40-6
• MW: 552.6
• Purity: >98%
• Formula: C₃₂H₃₂N₄O₅
• SMILES: Cc1ccc(NC(=O)c2ccc3OCCOc3c2)cc1NC(=O)c1ccc2nc(OCCN3CCCC3)ccc2c1
• Target: Transcription factor
• Solubility: Soluble in DMSO (up to 5 mg/ml).

Bioactivity

• Target IC50:
  HSP72:19 nM
• In Vivo:
  CCT367766 (oral; 20 mg/kg; 33 days) showed significant efficacy in mice, with a tumor growth inhibition (%TGI) of 70% based on final tumor volume.After 33 days, there was a 64% reduction in mean tumor weight compared to controls. In addition, the basicity and high volume of distribution of the compound was observed in tumors up to a concentration of 940 nM .CCT367766 (oral, 5 or 20 mg/kg) showed free Cav0-24h values of 2.0 nM and 1.2 nM, respectively, in tumor-free immune-competent BALB/c mice ; and, in a mouse model of human myeloma xenografts, the CCT251236 (20 mg/kg, po) inhibited the HSF1 pathway and exhibited antimyeloma efficacy in a human myeloma xenograft mouse model .
• In Vitro:
  CCT367766 (0-100 nM; 24 hours) inhibited 17-AAG-induced HSF1-mediated expression of heat shock proteins HSP72 and HSP27 in SK-OV-3 cells in a concentration-dependent manner; CCT367766 also blocked 17-AAG-induced HSPA1A mRNA in a dose-dependent manner; in addition, CCT367766 (0-100 nM; 24 hours) exhibited an ideal balance of in vitro properties while maintaining good cell viability, with pIC50=7.73±0.07 (IC50=19 nM) for inhibiting HSF1-mediated HSP72 induction; in SK-OV-3 cells, the free GI50 was 1.1 nM.

Storage & Handling

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

Alternative Names

CCT251236, CCT-251236, CCT 251236, HSF1, HSP72, SK-OV-3 cells

Compound Identifiers

PubChem CID

117996749