Ridaforolimus (Deforolimus, MK8669, AP23573)

This product is for research use only, not for human use. We do not sell to patients.

For small sizes, please check our retail website as below: www.invivochem.com

Size	Price	Stock
250mg	$539	Check With Us
500mg	$799	Check With Us
1g	$1199	Check With Us

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Cat #: V0184 CAS #: 572924-54-0 Purity ≥ 98%

Description: Ridaforolimus (also known as deforolimus, AP-23573; MK-8669) is a novel, potent, investigational and selective mTOR inhibitor with significant antitumor effects.

References: Rivera VM, et al. Deforolimus (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.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	990.21
Molecular Formula	C53H84NO14P
CAS No.	572924-54-0
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 198 mg/mL (200 mM)r
	Water: <1 mg/mLr
	Ethanol: <1 mg/mL
SMILES Code	O=P(C)(C)O[C@H]1[C@H](OC)C[C@H](C[C@H]([C@H](CC([C@H](C)/C=C(C)/[C@@H](O)[C@H]2OC)=O)OC([C@]3([H])CCCCN3C(C([C@@](O4)(O)[C@H](C)CC[C@@]4([H])C[C@H](OC)/C(C)=C\C=C\C=C\[C@@H](C)C[C@@H](C)C2=O)=O)=O)=O)C)CC1
Synonyms	Deforolimus, Ridaforolimus; AP23573; AP 23573; AP-23573; MK8669; MK 8669; MK-8669;

Protocol	In Vitro	Treatment of HT-1080 fibrosarcoma cells with Ridaforolimus 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 Ridaforolimus reduces the proliferation of cell lines representing a variety of tumor types. Administration of Ridaforolimus to tumor cells in vitro elicit dose-dependent inhibition of mTOR activity with concomitant effects on cell growth and division. Ridaforolimus 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.
Protocol	In Vivo	Ridaforolimus inhibits tumor growth in mice bearing PC-3 (prostate), HCT-116 (colon), MCF7 (breast), PANC-1 (pancreas), or A549 (lung) xenografts. Ridaforolimus 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.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	1.0099 mL	5.0494 mL	10.0989 mL	20.1977 mL
5mM	0.2020 mL	1.0099 mL	2.0198 mL	4.0395 mL
10mM	0.1010 mL	0.5049 mL	1.0099 mL	2.0198 mL
20mM	0.0505 mL	0.2525 mL	0.5049 mL	1.0099 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

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