572924-54-0

572924-54-0 structure

Name: Ridaforolimus (Deforolimus, MK-8669)
Chemical Name: ridaforolimus
CAS Number: 572924-54-0
Molecular Formula: C₅₃H₈₄NO₁₄P
Molecular Weight: 990.206
Catalog: Biochemical Inhibitor PI3K/Akt/mTOR inhibitor (PI3K/Akt/mTOR) mTOR inhibitor
Create Date: 2018-06-17 11:23:40
Modify Date: 2024-01-04 19:57:27
Deforolimus (AP23573; MK-8669) is a potent and selective mTOR inhibitor; inhibits ribosomal protein S6 phosphorylation with an IC50 of 0.2 nM in HT-1080 cells.

Name	ridaforolimus
Synonyms	(1R,2R,4S)-4-{(2R)-2-[(1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,35R)-1,18-Dihydroxy-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-2,3,10,14,20-pentaoxo-11,36-dioxa-4-azatricyclo[30.3.1.0] hexatriaconta-16,24,26,28-tetraen-12-yl]propyl}-2-methoxycyclohexyl dimethylphosphinate Phosphinic acid, P,P-dimethyl-, (1R,2R,4S)-2-methoxy-4-[(2R)-2-[(3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,26R,27R,34aS)-1,4,5,6,9,10,11,12,13,14,21,22,23,24,25,26,27,28,29,31,32,33,34,34a-tetracosahydro-9,27-dihydroxy-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-1,5,11,28,29-pentaoxo-23,27-epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontin-3-yl]propyl]cyclohexyl ester Deforolimus Ridaforolimus

Description	Deforolimus (AP23573; MK-8669) is a potent and selective mTOR inhibitor; inhibits ribosomal protein S6 phosphorylation with an IC50 of 0.2 nM in HT-1080 cells.
Related Catalog	Research Areas >> Cancer
Target	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].
Cell Assay	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].
Animal Admin	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].
References	[1]. 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. [2]. Brandt M, et al. mTORC1 Inactivation Promotes Colitis-Induced Colorectal Cancer but Protects from APC Loss-Dependent Tumorigenesis. Cell Metab. 2018 Jan 9;27(1):118-135.e8.

Density	1.2±0.1 g/cm3
Boiling Point	996.2±75.0 °C at 760 mmHg
Melting Point	95-98ºC
Molecular Formula	C₅₃H₈₄NO₁₄P
Molecular Weight	990.206
Flash Point	556.3±37.1 °C
Exact Mass	989.562927
PSA	211.31000
LogP	3.12
Vapour Pressure	0.0±0.6 mmHg at 25°C
Index of Refraction	1.539
Storage condition	Hygroscopic, -20?C Freezer, Under Inert Atmosphere

53123-88-9

1111-92-8

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Literature: US2004/73024 A1, ; Page 38 ;

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Literature: US2014/58081 A1, ; Paragraph 0047 ;