TAS4464 hydrochloride

Overview

TAS4464 hydrochloride is a long-acting, highly selective covalent inhibitor targeting NEDD8 -activating enzyme ( NAE ) ( IC 50 =0.955 nM), and also inhibits CAII with an IC 50 of 0.73 μM, which is less potent than MLN4924 ( HY-70062 ). The IC 50 values of TAS4464 hydrochloride against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 hydrochloride targets NEDD8 in an ATP-dependent manner to inhibit NAE , blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα ), and further induces tumor cell apoptosis . TAS4464 hydrochloride exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 hydrochloride has a wide therapeutic window, without obvious toxicity. TAS4464 hydrochloride can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer , colorectal cancer , sarcoma, endometrial cancer , ovarian cancer , etc.).

Application

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Product Information

• Catalog No.: HY-128586A
• CAS No.: 1848959-11-4
• Molecular Formula: C21H24ClFN6O6S
• Molecular Weight: 542.97
• Purity: 98.91%
• Storage: 4°C, sealed storage, away from moisture * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
• Solubility: ≥ 2.08 mg/mL (3.83 mM); Clear solution
• Availability: In-stock

Source

Original product source