1. PI3K/Akt/mTOR
  2. mTOR

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

Cat. No.: HY-50908 Purity: 98.46%
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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10 mg USD 92 In-stock
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Estimated Time of Arrival: December 31
50 mg USD 355 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
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Customer Review

View All mTOR Isoform Specific Products:

  • 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[1]

mTOR

 

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. In HT-1080 cells, the EC50 for inhibition of cell proliferation (0.5 nM) is similar to the EC50s for inhibition of S6 and 4E-BP1 phosphorylation. 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
References
Preparing Stock Solutions
Concentration Volume 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
Please refer to the solubility information to select the appropriate solvent.
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]

Mice: 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

SMILES

O=C([[email protected]@]1(O)[[email protected]@H](CC[[email protected]@H](C[[email protected]@H](/C(C)=C/C=C/C=C/[[email protected]](C[[email protected]@H](C)C([[email protected]@H]([[email protected]@H](/C(C)=C/[[email protected]]2C)O)OC)=O)C)OC)O1)C)C(N3CCCC[[email protected]]3C(O[[email protected]@H](CC2=O)[[email protected]@H](C[[email protected]@H]4C[[email protected]]([[email protected]](OP(C)(C)=O)CC4)OC)C)=O)=O

Storage
Powder -20°C 3 years
  4°C 2 years

*The compound is unstable in solutions, freshly prepared is recommended.

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 44 mg/mL

Deforolimus is dissolved in 1% DMSO in sunflower seed oil[2].

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

References

Purity: 98.46%

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Deforolimus
Cat. No.:
HY-50908
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