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PI3K-IN-2
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
PI3K-IN-2图片

PI3K-IN-2 (compound 10) 是一种口服有效的 PI3Kβ/δ 抑制剂 (IC50=7.1/8.6 nM)，与 PI3Kσ、PI3Kγ 相比 (IC50=13/190 nM)，选择性更好。
Canonical SMILESO=C1C=C(N2CCOCC2)OC3=C1C=C(C(N4CCCOC4)=O)C=C3[C@@H]5N(C6=CC(F)=CC(F)=C6)CCC5
分子式C28H29F2N3O5
分子量525.54
溶解度Soluble in DMSO
储存条件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
产品描述

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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