Uprosertib hydrochloride

A selective Akt inhibitor

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库存: 现货

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促销价

数量
5mg

￥1037.00

830.00

- +
10mg

￥1675.00

1340.00

- +
50mg

￥5937.00

4750.00

- +
100mg

￥7775.00

6220.00

- +
200mg

￥13350.00

10680.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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Background

Uprosertib is a selective, orally bioavailable inhibitor of Akt (IC₅₀s = 180, 328, and 38 nM for Akt1, Akt2, and Akt3, respectively).¹ Uprosertib preferentially inhibits the proliferation of human cancer cell lines with Akt pathway activation via PI3K/PTEN mutation or loss.² It can cause cell cycle arrest and consequent tumor growth inhibition in mice bearing either BT474 breast tumor or SK-OV-3 ovarian tumor xenografts.²

1.Pachl, F., Plattner, P., Ruprecht, B., et al.Characterization of a chemical affinity probe targeting Akt kinasesJ. Proteome Res.12(8)3792-3800(2013) 2.Dumble, M., Crouthamel, M.C., Zhang, S.Y., et al.Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitorPLoS One9(6)e100880(2014)

Protocol

Kinase experiment:

For selectivity profiling experiments, the lysates (5 mg of total protein each) are preincubated with 0 (DMSO control), 2.5 nM, 25 nM, 250 nM, 2.5 μM or 25 μM free compound (GSK690693 or Uprosertib) on an end-over-end shaker for 45 min at 4°C. Subsequently, lysates are incubated with beads (coupled Akt probe or kinobeads) for 1 h at 4°C, for both qualitative and quantitative experiments. The beads are washed with 1×CP buffer and collected by centrifugation. Bound proteins are eluted with 2×NuPAGE LDS sample buffer, and eluates are reduced and alkylated by 50 mM dithiothreitol and 55 mM iodoacetamide.

参考文献:

[1]. Pachl F, et al. Characterization of a chemical affinity probe targeting Akt kinases. J Proteome Res. 2013 Aug 2;12(8):3792-800.