CCT128930
目录号 : GC15864
An inhibitor of Akt2
Cas No.:885499-61-6
Sample solution is provided at 25 µL, 10mM.
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CCT128930 is a potent, selective, novel and ATP-competitive inhibitor for AKT2 (IC50= 6 nM). It also has 28-fold and 20-fold selectivity over PKA kinase (IC50= 168 nM) and p70S6K (IC50= 120 nM), respectively.
Akt (protein kinase B) is a serine/threonine-specific protein kinase that plays a key role in multiple cellular processes such as glucose metabolism, apoptosis, cell proliferation, transcription and cell migration.
In multi tumor cell line, CCT128930 showed antiproliferative effect and blocked the phosphorylation of various Akt substrates. In PTEN-null human glioblastoma cells (U87MG), CCT128930 treatment led to a G1 arrest associated with Akt pathway suppression. [1]
In U87MG tumor xenografts, CCT128930 inhibited the phosphorylation of Akt downstream biomarkers. In U87MG, HER-2 positive and IK3CA-mutant BT474 human breast cancer xenografts, antitumor activity were recorded as tumor volume decreased. CCT128930-treated mouse whisker folliciles in vivo and human hair follicles treated ex vivo exerted prominent reduction in pThr246 PRAS40. [1]
Reference:
1. Yap TA, Walton MI, Hunter LJ et al. Preclinical pharmacology, antitumor activity, and development of pharmacodynamic markers for the novel, potent AKT inhibitor CCT128930. Mol Cancer Ther. 2011 Feb;10(2):360-71.
Kinase experiment: | Profiling against 50 different human kinases is carried out using 10 μM CCT128930 at an ATP concentration equivalent to the Km for each enzyme. All other enzyme assays are performed[1]. |
Cell experiment: | All cell lines are grown in their recommended culture medium, supplemented with 10% fetal bovine serum at 37°C in 5% CO2 and passaged for less than six months prior to replacement from early passage frozen stocks. CCT128930 and LY294002 are made up as 10mM stocks in DMSO. Cells are regularly screened for Mycoplasma using a PCR-based assay. Cells are seeded in 96-well plates and allowed to attach for 36 hours to ensure exponential growth prior to treatment. In vitro antiproliferative activity is determined using a 96-hour SRB assay, and GI50 values are derived[1]. |
Animal experiment: | Mice[1] PTEN-null U87MG human glioblastoma cells (2×106) are injected subcutaneously (s.c.) in the right flank of 6-8 weeks old female CrTacNCr-Fox1nu mice. For HER2-positive, PIK3CA-mutant BT474 human breast cancer xenografts, cells (5×106) are administered s.c. in medium supplemented with matrigel (1:1) into the mammary fat pads of female mice implanted s.c. with estradiol pellets (0.025 mg, 90 day release) 3 days previously. Animals are randomized and treatment is started with vehicle or CCT128930 when established tumors are ~100 mm3 in mean volume. Control mice receive vehicle only (10% DMSO, 5% Tween 20, 85% saline) and treated mice received 50 mg/kg CCT128930 intraperitoneally (i.p.) daily for 5 days (U87MG human glioblastoma xenografts) or 40 mg/kg CCT128930 i.p. twice daily for 5 days (BT474 human breast cancer xenografts). Tumor size and body weight are monitored three times a week. Tumor size is evaluated by measurement of 2 orthogonal diameters with calipers and volume is calculated. At the end of the study, tumors are excised and weighed. |
References: [1]. Yap TA et al. Preclinical pharmacology, antitumor activity, and development of pharmacodynamic markers for the novel, potent AKT inhibitor CCT128930. Mol Cancer Ther. 2011 Feb;10(2):360-71. | |
| Cas No. | 885499-61-6 | SDF | |
| 化学名 | 4-[(4-chlorophenyl)methyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-4-amine | ||
| Canonical SMILES | C1CN(CCC1(CC2=CC=C(C=C2)Cl)N)C3=NC=NC4=C3C=CN4 | ||
| 分子式 | C18H20ClN5 | 分子量 | 341.84 |
| 溶解度 | ≥ 17.1mg/mL 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 | 2.9253 mL | 14.6267 mL | 29.2535 mL |
| 5 mM | 0.5851 mL | 2.9253 mL | 5.8507 mL |
| 10 mM | 0.2925 mL | 1.4627 mL | 2.9253 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
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- Purity: >99.50%
- COA (Certificate Of Analysis)
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