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Ridaforolimus

Catalog No. T6334   CAS 572924-54-0
Synonyms: AP23573, Deforolimus, MK-8669

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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Ridaforolimus Chemical Structure
Ridaforolimus, CAS 572924-54-0
Pack Size Availability Price/USD Quantity
5 mg In stock $ 51.00
10 mg In stock $ 81.00
25 mg In stock $ 165.00
50 mg In stock $ 297.00
1 mL * 10 mM (in DMSO) In stock $ 95.00
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Purity: 98.55%
Purity: 98%
Purity: 95%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 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.
Targets&IC50 mTOR (HT-1080 cells):0.2 nM
Kinase Assay 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).
Cell Research 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.
Animal Research 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
Synonyms AP23573, Deforolimus, MK-8669
Molecular Weight 990.21
Formula C53H84NO14P
CAS No. 572924-54-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 182 mg/mL (183.8 mM)

TargetMolReferences and Literature

1. Rivera VM, et al. Mol Cancer Ther, 2011, 10(6), 1059-1071. 2. Legrier ME, et al. Cancer Res, 2007, 67(23), 11300-11308. 3. Gayle SS, et al. Anticancer Agents Med Chem, 2012, 12(2), 151-162. 4. Squillace RM, et al. Int J Oncol, 2012, 41(2), 425-432. 5. Floc'h N, et al. Cancer Res, 2012, 72(17), 4483-4493. 6. Brandt M, et al. mTORC1 Inactivation Promotes Colitis-Induced Colorectal Cancer but Protects from APC Loss-Dependent Tumorigenesis. Cell Metab. 2018 Jan 9;27(1):118-135.e8.

TargetMolCitations

1. Chen W, Liao Y, Sun P, et al.Construction of an ER stress-related prognostic signature for predicting prognosis and screening the effective anti-tumor drug in osteosarcoma.Journal of Translational Medicine.2024, 22(1): 1-19.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Stem Cell Differentiation Compound Library Anti-Pancreatic Cancer Compound Library PI3K-AKT-mTOR Compound Library Anti-Cardiovascular Disease Compound Library Drug Repurposing Compound Library Bioactive Compounds Library Max Anti-Infection Compound Library

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Keywords

Ridaforolimus 572924-54-0 Autophagy PI3K/Akt/mTOR signaling mTOR inhibit AP23573 MK 8669 Deforolimus Mammalian target of Rapamycin Inhibitor MK8669 AP-23573 AP 23573 MK-8669 inhibitor

 

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