Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: sulfamic acid, [(1R,2R,3S,4R)-2,3-dihydroxy-4-[[2-[3-[(trifluoromethyl)thio]phenyl]pyrazolo[1,5-a]pyrimidin-7-yl]amino]cyclopentyl]methyl ester
Purity: ≥98%
Formula Markup: C19H20F3N5O5S2
Formula Weight: 519.520009
CAS Number: 1450833-55-2
Notes: MLN7243 is an inhibitor of ubiquitin-activating enzyme (UAE; IC50 = 1 nM).{52441} It is selective for UAE over NEDD8-activating enzyme (NAE), SUMO-activating enzyme (SAE), and the autophagy-activating enzyme ATG7 (IC50s = 28, 850, and >10,000 nM, respectively). MLN7243 inhibits proliferation in a panel of 30 cancer cell lines (EC50s = 0.006-1.1 µM). It activates the unfolded protein response (UPR) and expansion of the endoplasmic reticulum surface area, a marker of ER stress, in HCT116 cells. In vivo, MLN7243 (12.5-25 mg/kg) reduces tumor growth in WSU-DLCL2, HCT116, Calu-6, THP-1, CWR22, HCC70, and MM.1S mouse xenograft models, as well as patient-derived xenograft (PDX) mouse models of colon, lung, breast, ovarian, and neck cancer.
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