Formulation: A solid
Formal Name: (3R,3aS)-rel-1-([1,1′-biphenyl]-4-ylmethyl)-1,2,3,4,5,6-hexahydro-3-[2-(methylamino)-2-oxoethyl]-2-oxo-3aH-indole-3a-carboxylic acid, ethyl ester
Purity: ≥98%
Formula Markup: C27H30N2O4
Formula Weight: 446,5
Shelf life (days): 1460
CAS Number: 1644060-37-6
Notes: Fumarate hydratase-IN-1 is an antiproliferative and anti-inflammatory compound.{72414} It inhibits proliferation of, and induces ATP depletion in, SW620 colorectal, ACHN kidney, HCT116 colorectal, PC3 prostate, and SK-MEL-28 melanoma cancer cells in the absence, but not in the presence, of glucose in a concentration-dependent manner. Fumarate hydratase-IN-1 reduces the oxygen consumption rate (OCR) in SW620 cells in the absence of glucose (IC50 = 2.2 µM). Preincubation with fumarate hydratase-IN-1 (25 µM) reduces secretion of Ifn-γ, Tnf-α, and granzyme B from mouse CD8+ T cells when co-cultured with B16-OVA melanoma cells expressing ovalbumin.{72415} In vivo, fumarate hydratase-IN-1 (25 mg/kg per day) increases tumor interstitial fluid levels of fumarate and the percentage of apoptotic tumor-associated CD8+ T cells, as well as reduces the levels of tumor-associated CD44+ CD8+ T cells and survival, in a B16-OVA murine melanoma model.
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