Everolimus (RAD001) - Moligand™, 10mM in DMSO , FK506-binding protein 1A inhibitor, CAS No.159351-69-6, FK506-binding protein 1A inhibitor

CAS: 159351-69-6 Cat. No.: E409231 Molecular Weight: 958.25 EC Number: 621-003-9

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

SDZ-RAD

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

In vitro

Everolimus exhibits the immunosuppressive activity which is comparable to that of rapamycin. Everolimus competes with immobilized FK 506 for binding to biotinylated FKBP12 and shows the inhibitory effect on a two-way MLR performed with spleen cells from BALB/c and CBA mice with IC50 of 0.12-1.8 nM. Everolimus also shows antiangiogenic/vascular effects in VEGF-induced HUVEC proliferation with IC50 of 0.12 nM and bFGF-induced HUVEC proliferation with IC50 of 0.8 nM, respectively. A recent study shows that Everolimus shows a dose-dependent inhibitory effects on both the total cells and the stem cells from the BT474 cell line and the primary breast cancer cells with IC50 of 156 nM in total cells of primary breast cancer cells and 71 nM in total cells of BT474 cells. In addition, combination treatment with Everolimus and trastuzumab produces the significantly increased inhibition on the growth of cancer stem cells with the inhibition rate increased by more than 50 %.

In vivo

Everolimus (0.1 to 10 mg/kg) dose-dependently inhibits growth of the primary (ear) and lymph node metastases of B16/BL6 melanoma, with decreased total number of vessels and reduced mature vessels. In a xenograft animal model of BT474 stem cells, Everolimus shows significant reductions in mean tumor sizes (590.6 mm³), compared to the control group with a tumor size of 698 mm³. Furthermore, combination treatment with Everolimus and trastuzumab significantly decreases the xenograft tumor size (410.8 mm³) more than Everolimus treatment alone.
Cell Data

cell lines：

Concentrations：0.001-10 μM

Incubation Time：24 hours

Powder Purity:≥97%

Specifications

Synonyms

SDZ-RAD

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Everolimus (RAD001, SDZ-RAD) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM in a cell-free assay. Everolimus induces cell apoptosis and autophagy and inhibits tumor cells proliferation.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

FK506-binding protein 1A inhibitor

Product Properties

• ALogP: 5.9

Names and Identifiers

• 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)OCCO)C)/C)O)OC)C)C)/C)OC
• Molecular Weight: 958.25
• Reaxy-Rn: 28424947
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=28424947&ln=

Associated Targets(Human)

MTOR Tclin Serine/threonine-protein kinase mTOR (3 Activities)

Discover Target: MTOR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

References

1. Xiaoqian Jiang, Xinxin Xu, Hua Kuang, Liqiang Liu, Liguang Xu, Aihua Qu, Chuanlai Xu.  (2023)  A gold-based immunochromatographic strip for the specific detection of tacrolimus in whole blood.  Journal of Materials Chemistry B,  11  (20): (4464-4474).  [PMID:37159048] [10.1039/D3TB00569K]

2. Cui Jing, Guo Yao, Wu Heshui, Xiong Jiongxin, Peng Tao.  (2021)  Everolimus regulates the activity of gemcitabine-resistant pancreatic cancer cells by targeting the Warburg effect via PI3K/AKT/mTOR signaling.  MOLECULAR MEDICINE,  27  (1): (1-16).  [PMID:33849427] [10.1186/s10020-021-00300-8]

3. Fengqin Wang, Hanzhong Zhang, Zhigang Cheng.  (2021)  EPHA2 Promotes the Invasion and Migration of Human Tongue Squamous Cell Carcinoma Cal-27 Cells by Enhancing AKT/mTOR Signaling Pathway.  Biomed Research International,      [PMID:33834064] [10.1155/2021/4219690]

4. Yiqun Xia, Jundixia Chen, Yun Yu, Fengjiao Wu, Xin Shen, Chenyu Qiu, Tingting Zhang, Lin Hong, Peisen Zheng, Rongrong Shao, Chenxin Xu, Fang Wu, Wei Chen, Congying Xie, Ri Cui, Peng Zou.  (2021)  Compensatory combination of mTOR and TrxR inhibitors to cause oxidative stress and regression of tumors.  Theranostics,      [PMID:33754064] [10.7150/thno.52077]

5. Xin Wang, Feiyang Pu, Xuanye Yang, Xili Feng, Jiayou Zhang, Kai Duan, Xuanxuan Nian, Zhongren Ma, Xiao-Xia Ma, Xiao-Ming Yang.  (2024)  Immunosuppressants exert antiviral effects against influenza A(H1N1)pdm09 virus via inhibition on nucleic acid synthesis, mRNA splicing and protein stability.  Virulence,      [PMID:38170681] [10.1080/21505594.2023.2301242]

6. Qi Liu-Jie, Zhang Zhao-Qi, Iqbal Mujahid, Wang Fei, Li Jing-An, Guan Shao-Kang.  (2025)  Spraying-assisted layer-by-layer assembled coatings with dual self-healing ability to resist degradation and enhance endothelialization of ZE21B alloys for vascular stents.  RARE METALS,      [PMID:] [10.1007/s12598-024-03159-w]