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| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
CCT251236
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
CCT251236 is an orally available pirin ligand from a heat shock transcription factor 1 (hsf1) phenotypic screen with an IC 50 of 19 nM for inhibition of HSF1-mediated HSP72 induction.
In Vitro
CCT251236 (0-100 nM; 24hours) displays a desired balance of in vitro properties, while maintaining excellent cellular activity with a pIC50=7.73 ± 0.07 (IC 50 =19 nM) for inhibition of HSF1-mediated HSP72 induction. The free GI 50 is 1.1 nM in SK-OV-3 cells that calculated from the free fraction in the cell assay. CCT251236 (0-100 nM; 24 hours) blocks 17-AAG induced he HSF1-mediated heat-shock proteins, HSP72 and HSP27 expression as a concentration manner in SK-OV-3 cells. CCT251236 (0-100 nM; 24 hours), pre-treated with 250 nM 17-AAG for 6h, blocks the induction of HSPA1A mRNA by 17-AAG in a dosedependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: SK-OV-3 cells Concentration: 0 nM; 10 nM; 100 nM Incubation Time: 24 hours Result: Inhibited HSP72 and HSP27 expression at the dose of 10 nM. RT-PCRCell Line: SK-OV-3 cells Concentration: 0 nM; 10 nM; 100 nM and 1000 nM Incubation Time: 24 hours Result: Decreased HSPA1A mRNA level.
In Vivo
CCT251236 (oral adminstation; 5 or 20 mg/kg) in nontumor bearing immunocompetent BALB/c mice exhibits free C av 0-24h value of 2.0 nM and 1.2 nM, respectively. CCT251236 (oral adminstation; 20 mg/kg; 33 days) has a clear therapeutic efficacy in mice with a tumor growth inhibition (%TGI) of 70% based on final tumor volumes. After 33 days, the mean tumor weights decreases 64% when compares to control group. In addition, the compound’s basicity and high volume of distribution shows in tumor withtumor concentrations of CCT251236 as high as 940 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Athymic mice with SK-OV-3 cellsDosage: 20 mg/kg; 33 days Administration: Oral adminstation Result: Was efficacious in SK-OV-3 cell induced-tumor mice model.
IC50& Target:HSP72 19 nM (IC 50 , SK-OV-3 cells)
规格
规格或纯度
Moligand™, 10mM in DMSO
英文名称
CCT251236
生化机理
CCT251236 是通过热休克转录因子 1（hsf1）表型筛选获得的一种口服 pirin 配体，其抑制 HSF1 介导的 HSP72 诱导的 IC 50 为 19 nM。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
EC号
849-595-6
分子类型
小分子
Isomeric SMILES
CC1=C(C=C(C=C1)NC(=O)C2=CC3=C(C=C2)OCCO3)NC(=O)C4=CC5=C(C=C4)N=C(C=C5)OCCN6CCCC6
关联CAS
PubChem CID
MeSH Entry Terms
CCT251236
分子量
552.62
技术文档
高级数据
关联靶点（人）
HSF1
Tchem
热休克因子蛋白1(Heat shock factor protein 1)
(4 活性数据)
PIR
Tchem
皮林(Pirin)
(5 活性数据)
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:
溶液计算器
常见问题
本产品应如何储存？
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 1693731-40-6，分子式为 C32H32N4O5，分子量为 552.62 g/mol。
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