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Temsirolimus

现货
Catalog No.
A8314
mTOR抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,150.00
现货
10mg
¥ 850.00
现货
25mg
¥ 1,790.00
现货
50mg
¥ 2,590.00
现货
200mg
¥ 6,090.00
现货

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Background

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt1030.29
Cas No.162635-04-3
FormulaC56H87NO16
SynonymsTorisel;CCI-779;CCI 779;CCI779
Solubility≥51.5mg/mL in DMSO, ≥11.2 mg/mL in EtOH, <2.44 mg/mL in H2O
SDFDownload SDF
Canonical SMILESCO[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
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验: [1]

细胞系

PC-3和DU145 细胞

制备方法

该化合物在DMSO中的溶解度大于10 mM,若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应条件

100 nM,3 days

实验结果

在PC-3和DU145 细胞系中,CCI-779以浓度依赖性方式抑制细胞的生长和集落形成。使用100 nmol/L CCI-779处理3天后,与对照组相比,PC-3和DU145细胞的集落形成数目分别为0.18 ± 0.09和0.37 ± 0.03。

动物实验: [2]

动物模型

DAOY异种移植裸鼠

给药剂量

腹腔注射,20 mg/kg, 1、2或4周,每周5天;或在第1和12天注射100 mg/kg

实验结果

20 mg/kg CCI-779给药1和2周,5天/周,将肿瘤生长延迟1.6和2.4倍。与对照动物相比,治疗1周或2周的动物中达到5倍肿瘤体积所需时间更长。使用CCI-779对大肿瘤再治疗2周(20 mg/kg,i.p.,5天/周,第29至42天)恢复生长抑制,但不产生肿瘤消退。与对照相比,用CCI-779(20 mg/kg i.p.)5天/周治疗4周,将肿瘤体积生长至5倍的时间延迟174%。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

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.

生物活性

描述 Temsirolimus (CCI-779)是mTOR的一个特定的抑制剂,IC50值为1.76 μM。
靶点 mTOR          
IC50 1.76 μM          

质量控制

化学结构

Temsirolimus

相关生物数据

Temsirolimus

相关生物数据

Temsirolimus