CC-885

SKU: orb1308485

Description

CC-885 is a cereblon (CRBN) E3 ligase modulator with potent antitumor activity. It is widely used in cancer research, particularly in studies of targeted protein degradation, demonstrating efficacy in both in vitro and in vivo models for hematological and solid tumors.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1010100-07-8
• MW: 440.88
• Purity: 99.83% (May vary between batches)
• Formula: C₂₂H₂₁ClN₄O₄
• SMILES: O=C(NCC1=CC2=C(C(N(C(CC3)C(NC3=O)=O)C2)=O)C=C1)NC4=CC=C(C)C(Cl)=C4
• Target: Ligands for E3 Ligase,Molecular Glues
• Solubility: 10% DMSO+90% Corn Oil:2.5 mg/mL (5.67 mM);DMSO:67.5 mg/mL (153.1 mM)

Bioactivity

• In Vitro:
  CC-885 exhibits stronger antiproliferative effects than Lenalidomide and Pomalidomide across various cell types, including acute myeloblastic leukemia (AML) cell lines, THLE-2 human liver epithelial cells, and human peripheral blood mononuclear cells (PBMC), with IC50 values ranging from 10×-6-1 μM. The compound's efficacy was also assessed in 293T HEK cells engineered to express variants of GSPT1 that are either sensitive or resistant to CC-885. The study further explores the mechanism behind CC-885's cytotoxicity, particularly its dependency on cereblon-mediated degradation of GSPT1. By utilizing a GSPT1 mutant which maintains its functionality but lacks the cereblon binding affected by CC-885, the research distinguishes GSPT1's role from other potential targets. Notably, cells overexpressing the CC-885-resistant GSPT1 variant (GSPT1Δ(1–138)/(G575N)) were completely resistant to the compound's inhibitory effects on cell proliferation. In contrast, overexpressing a CC-885-sensitive variant (GSPT1Δ(1-138)) provided only partial protection against these effects, indicating the critical role of GSPT1 degradation in CC-885's mechanism of action. Similar outcomes were observed in AML cell lines.
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Storage & Handling

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

Alternative Names

Ligands for E3 Ligase, Ligand for E3 Ligase, LigandforE3Ligase, inhibit, Inhibitor, CRBN, E3 ligase-recruiting Moiety, CC 885, CC-885, CC885, cereblon

Compound Identifiers

PubChem CID

24788636