CI-994

SKU: orb1226959

Description

A potent, selective class I HDAC inhibitor with IC50 of 0.9/0.9/1.2 uM for HDAC1/2/3, respectively; show no significant inhibitory activity against HDAC8 (IC50>20 uM); reduces S phase level and increases apoptosis in A-549 and LX-1 cells; demonstrates antitumor activity against several tumor models, including the chemo-resistant mouse pancreatic ductal carcinoma as well as the human prostate tumor model LNCaP.Breast Cancer Phase 2 Discontinued(In Vitro):Tacedinaline (N-acetyldinaline) is a novel oral compound with a wide spectrum of antitumor activity in preclinical models. The mechanism of action may involve inhibition of histone deacetylation and cell cycle arrest. Tacedinaline (N-acetyldinaline) is combined with antineoplastic agents commonly used in non-small cell lung cancer cell line management, a marked synergism of action (R=1.8, R=1.5) is observed between Tacedinaline (N-acetyldinaline) (40 μM) and gemcitabine (0.01 μM) at 48 and 72 h of treatment. Tacedinaline (N-acetyldinaline) inhibits mitogen-stimulated blood lymphocyte proliferation with an IC50 value of 3 μM.\n(In Vivo):Tacedinaline (CI-994) has activity against 8/8 solid tumors tested: pancreatic ductal adenocarcinoma #02 (4.7); pancreatic adenocarcinoma #03 (3.0; 1/6 cures); colon adenocarcinoma #38 (1.6); colon adenocarcinoma #51/A (1.1); mammary adenocarcinoma #25 (1.7); mammary adenocarcinoma #17/ADR (0.5); Dunning osteogenic sarcoma (4.0); and the human prostate carcinoma LNCaP (1.2). CI-994 is the acetylated metabolite of dinaline and has the same spectrum of activity in vivo as dinaline. It also behaves similarly in schedule comparison/toxicity trials. Tacedinaline (CI-994) can effect lymphoid tissue in rats within 1 day of a single oral dose, that effects are generally reversible within 7 days.

Key Properties

• CAS Number: 112522-64-2
• MW: 269.2985
• Purity: >98% (HPLC)
• Formula: C₁₅H₁₅N₃O₂
• SMILES: O=C(NC1=CC=CC=C1N)C2=CC=C(NC(C)=O)C=C2
• Target: HDAC
• Solubility: DMSO: ≥ 58 mg/mL

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

Acetyldinaline | Tacedinaline | PD-123654 | Goe-5549

Quick Database Links

Gene Symbol

HDAC