质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
-10 to -25°C
SMILES字符串
N#CC1=CC2=C(C)C(CN3CCC(CC3)NC4=C5C=C(CC(F)(F)F)SC5=NC=N4)=CC=C2N1
生化/生理作用
MI-463 is an orally active and potent menin-MLL interaction inhibitor (cell-free IC50 = 15.3 nM against 1 nM FITC-MLL(4-13) peptide) that targets menin MLL-binding site with high affinity (KD = 9.9 nM by ITC). MI-463 selectively inhibits mixed lineage leukemia (MLL) oncogenic fusion-driven cancer progression in cultures (GI50 by MTT = 230 nM vs. >5 μM against murine BMCs with or without MLL-AF9 fusion transformation) and is efficacious against human MLL leukemia MV4;11 tumor growth in mice in vivo (35 mg/kg/day i.p.) and improve the survival of MLL leukemic mice (40-50 mg/kg b.i.d. p.o.).
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
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