Uprosertib hydrochloride
(Synonyms: GSK2141795 (hydrochloride)) 目录号 : GC37859
A selective Akt inhibitor
Cas No.:1047635-80-2
Sample solution is provided at 25 µL, 10mM.
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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)
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. | |
| Cas No. | 1047635-80-2 | SDF | |
| 别名 | GSK2141795 (hydrochloride) | ||
| Canonical 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 |
| 溶解度 | Soluble in DMSO | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1473 mL | 10.7363 mL | 21.4726 mL |
| 5 mM | 0.4295 mL | 2.1473 mL | 4.2945 mL |
| 10 mM | 0.2147 mL | 1.0736 mL | 2.1473 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet