1941174-13-5
中文名稱
L-Phenylalanine, 3-[[[2,4-dicyano-3-[4-[2-(methylamino)-2-oxoethoxy]phenyl]pyrido[1,2-a]benzimidazol-1-yl]amino]carbonyl]-
英文名稱
L-Phenylalanine, 3-[[[2,4-dicyano-3-[4-[2-(methylamino)-2-oxoethoxy]phenyl]pyrido[1,2-a]benzimidazol-1-yl]amino]carbonyl]-
CAS
1941174-13-5
分子式
C32H25N7O5
分子量
587.58
MOL 文件
1941174-13-5.mol
1941174-13-5 結(jié)構(gòu)式
基本信息
中文別名
化合物 T32404 英文別名
KMH-233L-Phenylalanine, 3-[[[2,4-dicyano-3-[4-[2-(methylamino)-2-oxoethoxy]phenyl]pyrido[1,2-a]benzimidazol-1-yl]amino]carbonyl]-
物理化學(xué)性質(zhì)
密度1.41±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO : 100 mg/mL (170.19 mM)
酸度系數(shù)(pKa)2.16±0.10(Predicted)
形態(tài)Solid
顏色White to yellow
常見問題列表
生物活性
KMH-233 是一種有效，可逆的且選擇性的 l 型氨基酸轉(zhuǎn)運蛋白 1 (LAT1) 抑制劑，可抑制LAT1底物，l-leucin 的攝取 (IC50=18 μM) 以及細(xì)胞生長。即使在低濃度 (25 μM) 下，KMH-233 仍可顯著增強 Bestatin 和順鉑的療效。體外研究
KMH-233 is able to inhibit binding and transport of essential neutral amino acids and thus, inhibit the cell growth of cancer cells.
KMH-233 shows a significant reduction of cell growth with an IC
50
of 124 μM.
KMH-233 is effective and able to potentiate the anti-proliferative efficacy of Bestatin (100 μM) and Cisplatin (100 μM) at a lower concentration of 25 μM, inhibiting cell growth 53% and 50%, respectively.
Cell Proliferation Assay
| Cell Line: | MCF-7 cells |
| Concentration: | 0.5-1000 μM |
| Incubation Time: | 72 hours |
| Result: | Showed a significant reduction of cell growth with an IC 50 of 124 μM. |