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TAK-243

Chemical Structure : TAK-243

CAS No.: 1450833-55-2

TAK-243 (MLN7243;MLN-7243;AOB87172;AOB-87172)

Catalog No.: PC-60178Not For Human Use, Lab Use Only.

TAK-243 (MLN-7243, AOB87172) is a small-molecule, cell-permeable inhibitor of ubiquitin-activating enzyme E1 (UAE1) with IC50 of 1 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

TAK-243 (MLN-7243, AOB87172) is a small-molecule, cell-permeable inhibitor of ubiquitin-activating enzyme E1 (UAE1) with IC50 of 1 nM.
TAK-243 blocks ssential monoubiquitination events within the translesion synthesis, and homologous recombination (HR) pathways.
TAK-243 shows synergistic and additive anti-tumor combination benefits in vivo combined with carboplatin and docetaxel.

Physicochemical Properties

M.Wt 519.514
Formula C19H20F3N5O5S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Methyl ((1S,2R,3S,4R)-2,3-dihydroxy-4-((2-(3-((trifluoromethyl)thio)phenyl)pyrazolo[1,5-a]pyrimidin-7-yl)amino)cyclopentyl)sulfamate

References

1. Wei J, et al. J Immunol. 2017 May 15;198(10):3835-3845.

2. Michael A. Milhollen, et al. DOI: 10.1158/1535-7163.

3. Barghout SH, et al. Leukemia. 2018 Jun 8. doi: 10.1038/s41375-018-0167-0.

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