1. PI3K/Akt/mTOR
  2. mTOR

Deforolimus (Synonyms: AP23573; MK-8669; Ridaforolimus)

Cat. No.: HY-50908 Purity: 98.46%
Data Sheet SDS Handling Instructions

Deforolimus (AP23573; MK-8669) is a potent and selective mTOR inhibitor; inhibits S6 phosphorylation with an IC50 of 0.2 nM in HT-1080 cells.

For research use only. We do not sell to patients.
Deforolimus Chemical Structure

Deforolimus Chemical Structure

CAS No. : 572924-54-0

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Deforolimus (AP23573; MK-8669) is a potent and selective mTOR inhibitor; inhibits S6 phosphorylation with an IC50 of 0.2 nM in HT-1080 cells.

IC50 & Target

IC50: 0.2 nM (HT-1080 cell)[1]

In Vitro

Treatment of HT-1080 fibrosarcoma cells with deforolimus results in a dose-dependent inhibition of phosphorylation of both S6 and 4E-BP1, with IC50s of 0.2 and 5.6 nM, respectively, and EC50s of 0.2 and 1.0 nM, respectively. Exposure to deforolimus reduces the proliferation of cell lines representing a variety of tumor types. Administration of deforolimus to tumor cells in vitro elicit dose-dependent inhibition of mTOR activity with concomitant effects on cell growth and division. Deforolimus exhibits a predominantly cytostatic mode of action, consistent with the findings for other mTOR inhibitors. Potent inhibitory effects on vascular endothelial growth factor secretion, endothelial cell growth, and glucose metabolism[1].

In Vivo

Deforolimus inhibits tumor growth in mice bearing PC-3 (prostate), HCT-116 (colon), MCF7 (breast), PANC-1 (pancreas), or A549 (lung) xenografts. Deforolimus inhibits tumor growth in a dose-dependent manner, with 0.3 mg/kg being the lowest dose that inhibits tumor growth significantly and 3 and 10 mg/kg doses achieving maximum inhibition[1].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00087451 Merck Sharp & Dohme Corp.|Ariad Pharmaceuticals Malignant Glioma|Glioblastoma|Gliosarcoma July 2004 Phase 1
NCT00087451 Merck Sharp & Dohme Corp.|Ariad Pharmaceuticals Malignant Glioma|Glioblastoma|Gliosarcoma July 2004 Phase 1
NCT01243762 Merck Sharp & Dohme Corp. Neoplasms Malignant November 2010 Phase 1
NCT00777959 Merck Sharp & Dohme Corp.|Ariad Pharmaceuticals Prostate Cancer October 2008 Phase 2
NCT00694083 Merck Sharp & Dohme Corp. Neoplasm June 2008 Phase 1
NCT01212627 Angela Taber MD|Rhode Island Hospital|The Miriam Hospital|Memorial Hospital of Rhode Island|Roger Williams Medical Center|Brown University Non-Small Cell Lung Cancer September 2010 Phase 1
NCT00112372 Merck Sharp & Dohme Corp.|Ariad Pharmaceuticals Cancer May 2005 Phase 1
NCT01431534 Merck Sharp & Dohme Corp. Solid Tumors January 30, 2012 Phase 1
NCT00093080 Merck Sharp & Dohme Corp.|Ariad Pharmaceuticals Leiomyosarcoma|Liposarcoma|Osteosarcoma|Sarcoma, Soft Tissue|Metastases October 2004 Phase 2
NCT00704054 Merck Sharp & Dohme Corp.|H. Lee Moffitt Cancer Center and Research Institute|Pediatric Cancer Foundation|University of Colorado, Denver|Johns Hopkins All Children's Hospital|Memorial Sloan Kettering Cancer Center Solid Tumors January 2008 Phase 1
NCT01296659 The University of Texas Health Science Center at San Antonio|Merck Sharp & Dohme Corp. Soft Tissue Sarcoma February 2011 Phase 1
NCT01010672 Merck Sharp & Dohme Corp.|Ariad Pharmaceuticals Sarcoma November 2009 Phase 2
NCT01380184 Merck Sharp & Dohme Corp. Cancer, Advanced July 2011 Phase 1
NCT01043887 Merck Sharp & Dohme Corp.|Ariad Pharmaceuticals Healthy Volunteers|Hepatic Insufficiency January 2010 Phase 1
NCT00122343 Merck Sharp & Dohme Corp.|Ariad Pharmaceuticals Endometrial Cancer August 2005 Phase 2
NCT00874731 Merck Sharp & Dohme Corp. Metastatic or Locally Advanced Cancer. April 2009 Phase 1
NCT00781846 Merck Sharp & Dohme Corp.|Ariad Pharmaceuticals Solid Tumor October 2008 Phase 1
NCT00836927 Merck Sharp & Dohme Corp.|Ariad Pharmaceuticals Advanced Cancers February 1, 2009 Phase 2
NCT00730379 Merck Sharp & Dohme Corp.|Ariad Pharmaceuticals Neoplasms July 2008 Phase 1
NCT00110188 Merck Sharp & Dohme Corp.|Ariad Pharmaceuticals Prostate Cancer May 2005 Phase 2
NCT00086125 Merck Sharp & Dohme Corp.|Ariad Pharmaceuticals Hematologic Malignancies|Leukemia|Myelodysplastic Syndromes|Myeloid Metaplasia|Lymphoma June 2004 Phase 2
NCT00736970 Merck Sharp & Dohme Corp. Breast Cancer|Breast Neoplasms July 2008 Phase 2
NCT00739830 Merck Sharp & Dohme Corp. Endometrial Cancer August 2008 Phase 2
NCT00818675 Merck Sharp & Dohme Corp.|Ariad Pharmaceuticals Non-Small Cell Lung Cancer March 2009 Phase 2
NCT00288431 Merck Sharp & Dohme Corp.|Ariad Pharmaceuticals Cancer|Sarcoma February 2006 Phase 1
NCT01431547 Merck Sharp & Dohme Corp. Solid Tumors February 2012 Phase 1
NCT00060645 Merck Sharp & Dohme Corp.|Ariad Pharmaceuticals Tumors|Lymphoma|Multiple Myeloma May 2003 Phase 1
NCT00060632 Merck Sharp & Dohme Corp.|Ariad Pharmaceuticals Tumors|Lymphoma|Multiple Myeloma April 2003 Phase 1
NCT01071304 Merck Sharp & Dohme Corp. Relapsed or Refractory Advanced Cancer March 2010 Phase 1
NCT01295632 Merck Sharp & Dohme Corp. Advanced Cancer February 2011 Phase 1
NCT01220570 Merck Sharp & Dohme Corp. Breast Cancer September 2010 Phase 1
NCT00770185 NCIC Clinical Trials Group|Canadian Cancer Trials Group Endometrial Cancer August 2008 Phase 2
NCT00538239 Merck Sharp & Dohme Corp.|Ariad Pharmaceuticals Metastatic Soft-Tissue Sarcomas|Metastatic Bone Sarcomas October 2007 Phase 3
NCT01256268 H. Lee Moffitt Cancer Center and Research Institute|Merck Sharp & Dohme Corp. Endometrial Cancer|Ovarian Cancer June 13, 2011 Phase 1
NCT01234857 Merck Sharp & Dohme Corp. Breast Cancer September 17, 2010 Phase 2
NCT01169532 Fox Chase Cancer Center|National Cancer Institute (NCI) Lymphoma|Unspecified Adult Solid Tumor, Protocol Specific October 2010 Phase 1
NCT01605396 Merck Sharp & Dohme Corp. Breast Neoplasms July 4, 2012 Phase 2
NCT02828917 Medinol Ltd. de Novo or Restenosis Lesions January 16, 2017
NCT02736344 Medinol Ltd. Heart Disease April 2016 Phase 3
NCT02834806 Medinol Ltd. Stenosis September 2016
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.0099 mL 5.0494 mL 10.0989 mL
5 mM 0.2020 mL 1.0099 mL 2.0198 mL
10 mM 0.1010 mL 0.5049 mL 1.0099 mL
Cell Assay
[1]

Cells are treated with 10-fold serial dilutions of deforolimus (1,000 to 0.0001 nM) or vehicle (ethanol). Following 72 hours culture at 37°C, the plates are aspirated and stored at −80°C for proliferation analysis[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mouse: Animals selected with tumors in the proper size range are assigned to various treatment groups. Deforolimus, at dosages of 3 and 10 mg/kg, is administered i.p. on 2 different treatment schedules: (a) daily, 5 continuous days every other week and (b) once weekly. The control group is untreated[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

990.21

Formula

C₅₃H₈₄NO₁₄P

CAS No.

572924-54-0

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 44 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.46%

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Deforolimus
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HY-50908
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