產品屬性:
產品名稱 | PI3K-IN-2 |
規格 | 1mg、5mg |
貨號 | EY-01Y17257 |
Cas No.: N/A
別名: N/A
化學名: N/A
分子式: C28H29F2N3O5

分子量: 525.54
溶解度: Soluble in DMSO
儲存條件: Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產品描述:
PI3K-IN-2 (compound 10) is a potent and orally active PI3Kβ/δ (IC50=7.1/8.6 nM) inhibitor with excellent selectivity versus PI3Kσ and PI3Kγ (IC50=13/190 nM, respectively)[1].
PI3Kα|13 nM (IC50)|PI3Kβ|7.1 nM (IC50)|PI3Kδ|190 nM (IC50)|PI3Kγ|8.6 nM (IC50)
PI3K-IN-2 (compound 10) shows PI3Kβ cell IC50 1.1 nM in phosphatase and tensin homolog (PTEN) null MDA-MB-468 cell and PI3Kδ cell IC50 14 nM in Jeko-1 B-cell[1].PI3K-IN-2 shows profound pharmacodynamic modulation of AKT phosphorylation in PTEN-deficient PC3 prostate tumour bearing mice after oral administration and gave significant inhibition of tumour growth in the same xenograft model[1].[1]. Barlaam B, et al. Discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-one as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours. Bioorg Med Chem Lett. 2017 May 1;27(9):1949-1954.
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