N-[(4-ピリジニル)メチル]-3-(4-クロロフェニル)アダマンタン-1-カルボアミド 化学特性,用途語,生産方法
説明
ABC294640 is an inhibitor of sphingosine kinase 2 (SPHK2; K
i = 9.8 μM). It inhibits SPHK2 (IC
50 = 60 μM) without affecting SPHK1 activity up to 100 μM but does reduce SPHK1 isoform a (SPHK1a) protein levels in androgen-independent LNCaP (LNCaP-AI) cells
via an SPHK1-indirect, proteasomal-dependent mechanism when used at concentrations ranging from 5 to 25 μM. ABC294640 is inactive against a panel of 20 lipid-regulated kinases at 50 μM. It decreases sphingosine-1-phosphate (S1P) production in MDA-MB-231 cells in a concentration-dependent manner. ABC294640 inhibits proliferation of a variety of cancer cells, including HepG2 liver, A-498 kidney, PANC-1 pancreas, and HT-29 colon cells (IC
50s = 6, 12.2, 32.8, and 48.1 μM, respectively). It reduces actin filament polymerization in, and cell migration of, A-498 cells in a scratch assay. Oral administration of ABC294640 (35 and 100 mg/kg every other day) reduces tumor growth in a mouse syngeneic model of mammary adenocarcinoma. It also reduces colonic inflammation in mouse and rat models of Crohn’s disease induced by trinitrobenzene sulfonic acid (TNBS).
使用
Opaganib is used in treating iatrogenic autoimmune colitis.
N-[(4-ピリジニル)メチル]-3-(4-クロロフェニル)アダマンタン-1-カルボアミド 上流と下流の製品情報
原材料
準備製品