Home >> Ridaforolimus (Deforolimus, MK-8669)
Related Products
Ridaforolimus (Deforolimus, MK-8669) MTOR inhibitor

Catalog No.B1639
Size Price Stock Qty
10mM (in 1mL DMSO)
$85.00
In stock
10mg
$73.00
In stock
50mg
$290.00
In stock
200mg
$554.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

      

Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

Ridaforolimus (Deforolimus, MK-8669)

Protocol

Kinase experiment [1]:

Cell based target inhibition

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 HRP-conjugated 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 from the inhibition of levels of phosphorylated ribosomal protein S6 (p-S6) and 4E-BP1 (p-4E-BP1).

Cell experiment:

Cell lines

HCT-116, SK-UT-1, HT-1080, SW872, MCF7, SK-LMS-1, U-87, A-204, PC-3, Endothelial cells, SK-UT-1B, ARK1 and ARK2 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

100 nmol/L for 24-72 hours; or 10–100 nM for 24 h.

Applications

Ridaforolimus showed the broad inhibitory effects on cell growth, division, metabolism, and angiogenesis and attenuated mTOR signaling [1]. Moreover, Ridaforolimus (20–100 nM) treatment decreased the viability in ARK1 and ARK2 cells [2].

Animal experiment:

Animal models

Female C57bl/6 and BALB/c mice model; male and female athymic NCr-nu mice model; mice harboring uterine serous carcinoma (USC) xenografts

Dosage form

3 or 10 mg/kg, i.p. daily for 5 days every other week or once weekly for 20 days; or 1 mg/kg, i.p. for 22 days

Applications

Ridaforolimus induced tumor growth inhibition in mice bearing PC-3 (prostate), HCT-116 (colon), MCF7 (breast), PANC-1 (pancreas), SK-LMS-1 (sarcoma) or A549 (lung) xenografts [1]. Moreover, Ridaforolimus improved the anti-tumor activity of dual HER2 blockade in mice harboring uterine serous carcinoma (USC) xenografts [2].

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

1. Rivera, V. M., Squillace, R. M., Miller, D., Berk, L., Wardwell, S. D., Ning, Y., Pollock, R., Narasimhan, N. I., Iuliucci, J. D., Wang, F. and Clackson, T. (2011) Ridaforolimus (AP23573; MK-8669), a potent mTOR inhibitor, has broad antitumor activity and can be optimally administered using intermittent dosing regimens. Mol Cancer Ther. 10, 1059-1071

2. Hernandez, S. F., Chisholm, S., Borger, D., Foster, R., Rueda, B. R. and Growdon, W. B. (2016) Ridaforolimus improves the anti-tumor activity of dual HER2 blockade in uterine serous carcinoma in vivo models with HER2 gene amplification and PIK3CA mutation. Gynecol Oncol. 141, 570-579

Ridaforolimus (Deforolimus, MK-8669) Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

Ridaforolimus (Deforolimus, MK-8669) Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Chemical Properties

Cas No. 572924-54-0 SDF Download SDF
Canonical SMILES O=P(C)(C)O[[email protected]]1[[email protected]](OC)C[[email protected]](C[[email protected]@H](C)[[email protected]@H](OC([[email protected]@H]2CCCCN2C(C([[email protected]]3([[email protected]@H](CC[[email protected]@H](C[[email protected]](OC)/C(C)=C/C=C/C=C/[[email protected]@H](C)C[[email protected]@H](C)C([[email protected]](OC)[[email protected]@H]4O)=O)O3)C)O)=O)=O)=O)CC([[email protected]](C)/C=C4\C)=O)CC1
Formula C53H84NO14P M.Wt 990.21
Solubility >49.5mg/ml in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

Ridaforolimus (Deforolimus, MK-8669), a novel rapamycin analogue, is a novel, potent and selective inhibitor of mTOR with IC50 value of 0.2nM [1].

HT-1080 fibrosarcoma cells treated with ridaforolimus have been demonstrated to dose-dependently inhibit S6 and 4E-BP1 phosphorylation with IC50 values of 0.2 and 5.6 nM, respectively, and EC50 values of 0.2 and 1.0 nM, respectively. The antiproliferative activity of ridaforolimus has been observed in a broad panel of cell lines including the colon cancer cells HCT-116, leiomyosarcoma cells SK-UT-1, etc. Ridaforolimus has shown to block the production of VEGF production dose-dependently, with an EC50 value of 0.1nM [1].

In vivo, mice bearing MCF7 (breast), PC-3 (prostate), A549 (lung), HCT-116 (colon) or PANC-1 (pancreas) xenografts have revealed the antitumor efficacy of ridaforolimus [1].

References:
[1] Rivera VM1, Squillace RM, Miller D, Berk L, Wardwell SD, Ning Y, Pollock R, Narasimhan NI, Iuliucci JD, Wang F, Clackson T.Ridaforolimus (AP23573; MK-8669), a potent mTOR inhibitor, has broad antitumor activity and can be optimally administered using intermittent dosing regimens. Mol Cancer Ther. 2011 Jun;10(6):1059-71.