TAK-243 (MLN7243), Ubiquitin Activating Enzyme (UAE) Inhibitor


Catalog No. size PriceQuantity
M60332-2S 2 mg solid $129
M60332-10S 10 mg solid $529

Description

Product Information
Molecular Weight: 519.52
Formula: C19H20F3N5O5S2
Purity: ≥98%
CAS#: 1450833-55-2
Solubility: DMSO up to 100 mM
Chemical Name:

((1R,2R,3S,4R)-2,3-dihydroxy-4-(2-(3-(trifluoromethylthio)phenyl)pyrazolo[1,5-a]pyrimidin-7-ylamino)cyclopentyl)methyl sulfamate

Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

TAK-243 (MLN7243) is a potent, selective and cell permeable small molecule inhibitor of the ubiquitin activating enzyme (UAE) at nM range. The ubiquitin-activating enzymes, found more active in cancer cells than in normal healthy cells, catalyze the first step in ubiquitination reaction, targeting a protein for degradation via proteasome. TAK-243 treatment caused depletion of cellular ubiquitin conjugates, resulting in disruption of signaling events, induction of proteotoxic stress, and impairment of cell cycle progression and DNA damage repair pathways. TAK-243 treatment caused death of cancer cells and, in primary human xenograft
studies, demonstrated antitumor activity at tolerated doses. Due to its specificity and potency, TAK-243 allows for interrogation of ubiquitin biology and for assessment of UAE inhibition as a new approach for cancer treatment. TAK-243 is now in phase I clinical trials for adult patients with advanced solid tumors.

How to Use:


In vitro: TAK-243 was suggested to be used at 1-10 µM final concentration in vitro and in cellular assays.
In vivo: TAK-243 was administered intravenously at 12.5-25 mg/Kg to a panel of human-patient-derived and cell-line-derived xenograft (PDX and CDX, respectively) tumor models on a twice-per-week schedule.

Reference:

  • 1. Hyer ML, et al. A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment. (2018) Nat Med. In press. 



  

Products are for research use only. Not for human use. 

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