Temsirolimus
(Synonyms: 西罗莫司脂化物,Torisel;CCI-779;CCI 779;CCI779) 目录号 : GC12573
A specific inhibitor of mTOR activity
Cas No.:162635-04-3
Sample solution is provided at 25 µL, 10mM.
CCI-779 is a potent inhibitor of mTOR with IC50 values of 0.6, 0.7, 0.7 and 50 nM for BT-474, MDA-MB-468, SKBR-3 and MCF-7 cells, respectively [1].
CCI-779 is an ester derivative of rapamycin and has improved pharmaceutical properties. As a mTOR inhibitor, CCI-779 affected cell proliferation in cancer cells in which the cell cycle targets are dysregulated by mTOR. When treated with a panel of 8 human breast cancer cell lines, CCI-779 showed potent antigrowth activity with IC50 values of 0.6, 0.7 and 0.7nM for BT-474, MDA-MB-468 and SKBR-3 cells, respectively. In mice bearing MDA-468 or MDA-435 xenografts, administration of CCI-779 significantly induced the regression of MDA-468 tumors but showed no effect on MDA-435 tumors, suggesting that CCI-779 was effect in PTEN mutant cells but not PTEN wild-type cells. CCI-779 also inhibited the growth of MCF-7 cells with IC50 value of 50 nM. Besides that, CCI-779 was also found to significantly inhibit cell growth in mice bearing myeloma tumors [1, 2].
References:
[1] Yu K, Toral-Barza L, Discafani C, et al. mTOR, a novel target in breast cancer: the effect of CCI-779, an mTOR inhibitor, in preclinical models of breast cancer. Endocrine-related cancer, 2001, 8(3): 249-258.
[2] Frost P, Moatamed F, Hoang B, et al. In vivo antitumor effects of the mTOR inhibitor CCI-779 against human multiple myeloma cells in a xenograft model. Blood, 2004, 104(13): 4181-4187.
| Cell experiment: [1] | |
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Cell lines |
PC-3 and DU145 cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
100 nM, 3 days |
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Applications |
The growth and colony-formation of both cell lines were inhibited in a concentration-dependent manner by CCI-779. Following a 3-day exposure to 100 nmol/L CCI-779, the numbers of colony-forming PC-3 and DU145 cells were 0.18 ± 0.09 and 0.37 ± 0.03, respectively, compared with controls. |
| Animal experiment: [2] | |
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Animal models |
Nude mice bearing DAOY xenografts |
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Dosage form |
Intraperitoneal injection, 20 mg/kg, daily 3 5 for 1, 2 or 4 weeks or 100 mg/kg on days 1 and 12 |
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Applications |
CCI-779 administered at 20 mg/kg 5 days/week for 1 and 2 weeks yielded 1.6- and 2.4-fold delayed tumor growth. Time to reach 5-fold tumor volume was significantly greater in animals treated for 1 week or 2 weeks compared with control animals. Retreatment of large tumors with CCI-779 for 2 weeks (20 mg/kg i.p. 5 days/week on days 29 to 42) restored growth inhibition but did not yield tumor regression. Treatment with CCI-779 (20 mg/kg i.p.) 5 days/week for 4 weeks delayed time to reach 5-fold pretreatment volume by 174% compared with controls. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Wu L, Birle D C, Tannock I F. Effects of the mammalian target of rapamycin inhibitor CCI-779 used alone or with chemotherapy on human prostate cancer cells and xenografts. Cancer research, 2005, 65(7): 2825-2831. [2] Geoerger B, Kerr K, Tang C B, et al. Antitumor activity of the rapamycin analog CCI-779 in human primitive neuroectodermal tumor/medulloblastoma models as single agent and in combination chemotherapy[J]. Cancer research, 2001, 61(4): 1527-1532. | |
| Cas No. | 162635-04-3 | SDF | |
| 别名 | 西罗莫司脂化物,Torisel;CCI-779;CCI 779;CCI779 | ||
| Canonical SMILES | CO[C@@H]1C[C@H](C[C@@H](C)[C@@H](OC([C@]2([H])CCCCN2C(C([C@]3(O)O[C@@](C[C@H](OC)/C(C)=C/C=C/C=C/[C@H](C[C@@H](C)C4=O)C)([H])CC[C@H]3C)=O)=O)=O)CC([C@H](C)/C=C(C)/[C@@H](O)[C@H]4OC)=O)CC[C@H]1OC(C(CO)(C)CO)=O | ||
| 分子式 | C56H87NO16 | 分子量 | 1030.29 |
| 溶解度 | ≥ 51.5mg/mL in DMSO, ≥ 11.2 mg/mL in EtOH | 储存条件 | 4°C, protect from light, stored under nitrogen |
| 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 | 0.9706 mL | 4.853 mL | 9.706 mL |
| 5 mM | 0.1941 mL | 0.9706 mL | 1.9412 mL |
| 10 mM | 0.0971 mL | 0.4853 mL | 0.9706 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet