ATR-101

SKU: orb1941097

Description

ATR-101 (PD-132301, Nevanimibe) is a selective and potent inhibitor of ACAT1 with IC50 of 52 nM; induces H295R cell apoptosis, causes mitochondrial hyperpolarization, reactive oxygen release, and ATP depletion, caspase-3/7 activation, and membrane permeabilization; decreases the formation of cholesteryl esters and increases FC levels in H295R adrenocortical carcinoma cells; inhibits the establishment and impeds the growth of ACC-derived H295R cell xenografts in mice; orally active.Cushing Disease Phase 2 Clinical(In Vitro):Coincubation of Nevanimibe hydrochloride (PD-132301 hydrochloride; ATR101 hydrochloride; 3 nM-30 μM) and Cholesterol markedly increases toxicity in a dose-dependent manner, where 3 nM Nevanimibe in the presence of 60 μg/mL Cholesterol reduces survival by 60% after 24 hours. All doses of Nevanimibe (3 nM-30 μM) induces cytoxicity in the presence of Cholesterol, whereas treatment with Cholesterol in the absence of Nevanimibe has no effect on cell viability.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 133825-81-7
• MW: 458.09
• Purity: >98% (HPLC)
• Formula: C₂₇H₄₀ClN₃O
• SMILES: CC(C)C1=C(C(=CC=C1)C(C)C)NC(=O)NCC2(CCCC2)C3=CC=C(C=C3)N(C)C.Cl
• Target: Other Targets
• Solubility: DMSO : 41.67 mg/mL. 90.97 mM

Bioactivity

• In Vitro:
  Cell Cytotoxicity Assay Cell line: The H295R and HAC clone 15 (HAC15) human ACC cell lines. Concentration: 3 nM-30 μM. Incubation time: 24 hours. Result: 3 nM-3 μM exhibited no toxicity, whereas 30 μM treatment reduced survival by approximately 40% within 24 hours.
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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

PD-132301 | PD132301-2 | ATR 101 | Nevanimibe

Quick Database Links

Gene Symbol

Other Targets