计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
替西罗莫司, FK506 结合蛋白 1A 抑制剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Temsirolimus (CCI-779) 抑制mTOR激酶活性 IC50值为1.76 ± 0.15 μM。A potent inhibitor of FRAP (mTOR) kinase activity
Information
Temsirolimus (CCI-779) Temsirolimus (CCI-779, NSC 683864) is a specific mTOR inhibitor with IC50 of 1.76 μM in a cell-free assay. Temsirolimus induces autophagy and apoptosis .
In vitro
In the absence of FKBP12, Temsirolimus potently inhibits mTOR kinase activity with IC50 of 1.76 μM, similar to that of rapamycin with IC50 of 1.74 μM. Temsirolimus treatment at nanomolar concentrations (10 nM to <5 μM) displays a modest and selective antiproliferative activity via FKBP12-dependent mechanism, but can completely inhibit the proliferation of a broad panel of tumor cells at low micromolar concentrations (5-15 μM), involving FKBP12-independent suppression of mTOR signaling. Temsirolimus treatment at micromolar but not nanomolar concentrations (20 μM) causes a marked decline in global protein synthesis and disassembly of polyribosomes, accompanied by rapid increase in the phosphorylation of translation elongation factor eEF2 and the translation initiation factor eIF2A. Temsirolimus inhibits the phosphorylation of ribosomal protein S6, more potently in PTEN-positive DU145 cells than in PTEN-negative PC-3 cells, and inhibits cell growth and clonogenic survival of both cells in a concentration-dependent manner. Temsirolimus (100 ng/mL) potently inhibits proliferation and induces apoptosis in primary human lymphoblastic leukemia (ALL) cells.
In vivo
In the NOD/SCID xenograft models with human ALL, Temsirolimus treatment at 10 mg/kg/day produces a decrease in peripheral blood blasts and in splenomegaly Administration of Temsirolimus (20 mg/kg i.p. 5 days/week) significantly delays the growth of DAOY xenografts by 160% after 1 week and 240% after 2 weeks, compared with controls. Single high-dose of Temsirolimus (100 mg/kg i.p) treatment induces 37% regression of tumor volume within 1 week. Temsirolimus treatment for 2 weeks also delays the growth of rapamycin-resistant U251 xenografts by 148%. Inhibition of mTOR by Temsirolimus improves performance on four different behavioral tasks and decreases aggregate formation in a mouse model of Huntington disease. Administration of Temsirolimus induces significant dose-dependent, antitumor responses against subcutaneous growth of 8226, OPM-2, and U266 xenografts with ED50 of 20 mg/kg and 2 mg/kg for 8226 and OPM-2, respectively, which are associated with inhibited proliferation and angiogenesis, induction of apoptosis, and reduction in tumor cell size.
Cell Data
cell lines：
Concentrations：Dissolved in DMSO, final concentrations ~20 μM
Incubation Time：72 hours
Powder Purity:≥98%
规格
英文别名
NSC 683864 | Rapamycin, 42-[3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate]
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Temsirolimus (CCI-779)
生化机理
Temsirolimus（CCI-779，NSC 683864）是一种特异性 mTOR 抑制剂，在无细胞试验中的 IC50 值为 1.76 μM。Temsirolimus 可诱导自噬和细胞凋亡。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
FK506 结合蛋白 1A 抑制剂
名称和识别符
EC号
686-177-0
分子类型
小分子
Isomeric SMILES
C[C@@H]1CC[C@H]2C[C@@H](/C(=C/C=C/C=C/[C@H](C[C@H](C(=O)[C@@H]([C@@H](/C(=C/[C@H](C(=O)C[C@H](OC(=O)[C@@H]3CCCCN3C(=O)C(=O)[C@@]1(O2)O)[C@H](C)C[C@@H]4CC[C@H]([C@@H](C4)OC)OC(=O)C(C)(CO)CO)C)/C)O)OC)C)C)/C)OC
PubChem CID
分子量
1030.29
技术文档
高级数据
产品属性
| ALogP | 5.6 |
|---|
关联靶点（人）
MTOR
Tclin
丝氨酸/苏氨酸蛋白激酶 mTOR(Serine/threonine-protein kinase mTOR)
(1 活性数据)
安全和危险性（GHS）
信号词
危险
危险声明
H360FD: 可能损害生育能力； 可能会伤害未出生的孩子
H410: 对水生生物有剧毒并具有长期持续影响
WGK Germany
3
个人防护装备
dust mask type N95 (US), Eyeshields, Faceshields, Gloves
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
通过匹配包装上的批号来查找并下载产品的 COA，每批产品都进行了严格的验证，您可放心使用！
| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 A2303671 |
分析证书 | T408907 |
技术文档和文章
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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