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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mg $77 In-stock
50 mg $296 In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Featured Recommendations

  • 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
View MoreCollapse
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]

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%

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Deforolimus
Cat. No.:
HY-50908
Quantity: