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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-Taselisib
Taselisib

Chemical Structure : Taselisib

CAS No.: 1282512-48-4

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Taselisib (GDC-0032, GDC0032, RG-7604)

货号: PC-22488Not For Human Use, Lab Use Only.

Taselisib (GDC-0032) is a potent, selective inhibitor of PIK3CA (PI3Kα) with Ki of 0.29 nM and pAkt IC50 of 4 nM, 31-fold selective over PI3Kβ.

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50 mg ￥2580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Taselisib (GDC-0032) is a potent, selective inhibitor of PIK3CA (PI3Kα) with Ki of 0.29 nM and pAkt IC50 of 4 nM, 31-fold selective over PI3Kβ.
Taselisib (GDC-0032) maintains biochemical selectivity over the non-class I PI3Ks, with IC50 values for PI3K-C2 beta and hVPS34 measuring 292 and 374 nM, respectively.
Taselisib (GDC-0032) achieves a 1000-fold selectivity against a panel of potential off-targets.
Taselisib (GDC-0032) potently inhibits cell proliferation of MCF7-neo/HER2 cells with IC50 of 25 nM.
Taselisib (GDC-0032) (2.8 mg/kg) resulted in a similar decrease in Akt phosphorylation (59%).
Taselisib (GDC-0032) orally at 1.4, 2.8, 5.8, 11.25, or 22.5 mg/kg resulted in dose-dependent increase in TGI (19%, 76%, 95%, 103%, and 123%, respectively) and tumor regressions in the MCF7-neo/Her2 xenograft model grown in nude mice.

物理化学性质&存储条件

分子量 460.54
分子式 C24H28N8O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-(4-(2-(1-Isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide

参考文献

1. Zumsteg ZS, et al. Clin Cancer Res. 2016 Apr 15;22(8):2009-19.

2. Ndubaku CO, et al. J Med Chem. 2013 Jun 13;56(11):4597-610.

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