CB-5083

SKU: orb1226121

Description

CB-5083 is a potent, selective, orally bioavailable inhibitor of p97 AAA with IC50 of 11 nM, specifically targets D2 ATPase site of p97, shows 9.6, 128 and 158-fold less affinity for DNA-PK, mTOR and PIK3C3; causes accumulation of poly-ubiquitinated proteins, retention of ERAD substrates, and generation of irresolvable proteotoxic stress, leading to activation of the apoptotic arm of the unfolded protein response (UPR) in cancer cells; inhibits A549 cell viability with IC50 of 0.67 uM, induces the UPR and apoptosis in xenograft tumor models.Blood Cancer Phase 1 Clinical.

Key Properties

• CAS Number: 1542705-92-9
• MW: 413.4717
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₃N₅O₂
• SMILES: O=C(C1=CC=CC2=C1C=C(C)N2C3=NC(NCC4=CC=CC=C4)=C(COCC5)C5=N3)N.
• Target: p97
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Animal model: Nu/Nu nude female mice bearing established human tumor xenografts derived from HCT 116 colon. Dosage: 75 mg/kg. Administration: Administered orally using every day (qd) dosing, for 2 weeks. Result: Showed more profound antitumor activity.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CB5083 | CB 5083

Quick Database Links

Gene Symbol

p97