Uprosertib hydrochloride

目录号: GC37859纯度: >98%同义词: GSK2141795 (hydrochloride)

A selective Akt inhibitor

Cas No.: 1047635-80-2

规格	价格	库存	数量
5mg	¥855.00	现货	1
10mg	¥1,395.00	现货	1
50mg	¥4,950.00	现货	1
100mg	¥6,480.00	现货	1
200mg	¥11,250.00	现货	1

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文献被引

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Nature
641, 529–536 (2025)
Nature
628, 630–638 (2024)
Nature
632, 686–694 (2024)
Nature
618, 1017–1023 (2023)
Nature
610, 366–372 (2022)
Cell
187(9):2288-2304 (2024)
Cell
183(7):1867-1883 (2020)
Science
388(6745) (2025)
Science
387(6739) (2025)
Science
387(6734) (2025)
Cell Research
35, 97–116 (2025)
Cell Research
34, 683–706 (2024)
Cell Research
33, 273–287 (2023)
Cell Research
33, 546–561 (2023)
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33, 904–922 (2023)
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31, 1291–1307 (2021)

产品描述 Description

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)

实验参考方法 Experimental Reference Method

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.

References:

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

产品文档 Product Documents

Purity:>98%

COA SDS Data Sheet

化学性质Chemical Properties

CAS 号

1047635-80-2

同义词

GSK2141795 (hydrochloride)

SMILES

O=C(C1=CC(C2=C(Cl)C=NN2C)=C(Cl)O1)N[C@@H](CC3=CC=C(F)C(F)=C3)CN.Cl

分子式

C₁₈H₁₇Cl₃F₂N₄O₂

分子量

465.71 g/mol

溶解性

Soluble in DMSO

保存条件

Store at -20°C

General tips

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。

Shipping Condition

评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

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