化合物 Ridaforolimus|T6334|TargetMol

Ridaforolimus
572924-54-0

询价 1removed 起订

上海更新日期：2024-12-12

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产品详情:

中文名称：: 化合物 Ridaforolimus

英文名称：: Ridaforolimus

CAS号：: 572924-54-0

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 98.55%

产品类别：: 抑制剂

货号：: T6334

Product Introduction

Bioactivity

名称	Ridaforolimus
描述	Ridaforolimus (AP23573) is a small molecule and non-prodrug analogue of the lipophilic macrolide antibiotic rapamycin with potential antitumor activity. Ridaforolimus binds to and inhibits the mammalian target of rapamycin (mTOR), which may result in cell cycle arrest and, consequently, the inhibition of tumor cell growth and proliferation. Upregulated in some tumors, mTOR is a serine/threonine kinase involved in regulating cellular proliferation, motility, and survival that is located downstream of the PI3K/Akt signaling pathway.
细胞实验	Cell lines: Colo205,H1755,H1395,H1666,A549,H157,and H1703 cells. Concentrations: Dissolved in ethanol,final concentrations ~ 1 μM. Method: Cells are seeded at 2-3 ×104/mL,and serial dilutions of Deforolimus are added after 2 hours,for at least three cell doublings (72-120 hours).Deforolimus effects are measured by the CellTiter 96 Aqueous nonradioactive cell proliferation assay and Sulforhodamine B assays.
激酶实验	HT-1080 cells are treated with increasing concentrations of Deforolimus (0-100 nM) for 2 hours, prior to harvest. Cellular lysates are extracted in denaturing lysis buffer, resolved on SDS-PAGE and transferred to PVDF membranes. After blocking, membranes are incubated with primary antibodies for 1 hour, followed by appropriate HRPconjugated secondary antibodies for 1 hour at room temperature. Immunoreactive proteins are detected using enhanced chemiluminescence and autoradiography performed by exposure to X-ray film. IC50 is determined by the inhibition of levels of phosphorylated ribosomal protein S6 (p-S6) and 4E-BP1 (p-4E-BP1).
动物实验	Animal Models: Male and female athymic NCr-nu mice with xenografts established by subcutaneous implantation of PC-3,A549,HCT-116,MCF7,PANC-1 and SK-LMS-1 tumors. Formulation: Dissolved in ethanol,and diluted in a vehicle of 4% ethanol,5% Tween 80,and 5% propylene glycol. Dosages: ~10 mg/kg. Administration: Intraperitoneally injection
体外活性	Deforolimus以剂量依赖性方式在携带PC-3（前列腺）,HCT-116（结肠）,MCF7（乳房）,PANC-1（胰腺）或A549（肺）异种移植物的小鼠中发挥显著的抗肿瘤作用,在与抑制肿瘤生长相关的SK-LMS-1异种移植模型中抑制mTOR信号传导.
体内活性	Deforolimus剂量依赖性抑制HT-1080细胞中S6和4E-BP1磷酸化,IC50分别为0.2 nM和5.6 nM,EC50分别为0.2 nM和1.0 nM,且导致细胞尺寸减小,G1期细胞增多,抑制葡萄糖摄取,EC50为0.1-1 nM。Deforolimus作用于一组细胞系,具有显著抗增殖活性,EC50为0.2-2.3 nM。Deforolimus有效且选择性及剂量依赖性抑制VEGF产量,EC50为~0.1 nM。Deforolimus和MEK抑制剂CI-1040或 PD0325901联用作用于人肺癌细胞系,具有协同作用,这种作用存在剂量依赖性,这种作用与细胞增殖受抑制而非细胞凋亡增多相关,处理24小时后,抑制40%核糖体合成,且使多核糖体/染色单体比例下降。Deforolimus显著抑制人NSCLC细胞系（除了H157细胞）细胞生长,IC30为2.45-8.83 nM,而作用于H157细胞时,IC30 >20 nM。2.8-5.9 nM Deforolimus处理A549,H1703和H157细胞（除了表达mTORC1耐药变异的H1666）,使p70S6KThr389去磷酸化,提高A549和H1703细胞中pAKTser473和pAKTThr308磷酸化水平。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 182 mg/mL (183.8 mM)
关键字	inhibit \| Autophagy \| MK 8669 \| Mammalian target of Rapamycin \| mTOR \| Ridaforolimus \| Inhibitor \| MK8669 \| AP-23573 \| AP 23573
相关产品	Oxyresveratrol \| Guanidine hydrochloride \| Naringin \| Taurine \| Gefitinib \| Xylitol \| Hydroxychloroquine \| Curcumin \| Stavudine \| Myricetin \| Paeonol \| Sodium 4-phenylbutyrate

AP23573|||Deforolimus|||MK-8669|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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