RidaforolimusA selective FRAP (mTOR) inhibitor

Ridaforolimus (CAS 572924-54-0)

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Synonym: Rapamycin 42-(Dimethylphosphinate)
Application: A selective FRAP (mTOR) inhibitor
CAS Number: 572924-54-0
Purity: ≥99%
Molecular Weight: 990.21
Molecular Formula: C53H84NO14P
* Refer to Certificate of Analysis for lot specific data (including water content).
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Ridaforolimus (Deforolimus, AP23573, MK-8669) is a selective FRAP (mTOR) inhibitor (IC50 of 0.2 nM). Ridaforolimus used to treat HT-1080 cells induces a dose-dependent inhibition of both S6 and 4E-BP1 phosphorylation, with IC50 of 0.2 nM and 5.6 nM, respectively, and leads to a decrease in cell size, an increase in the proportion of cells in the G1 phase of the cell cycle, and inhibition of glucose uptake. Ridaforolimus shows antiproliferative activity a variety of cell lines with EC50 of 0.2-2.3 nM. Ridaforolimus is a potent and selective inhibitor of VEGF production in a dose-dependent manner. Ridaforolimus treatment causes growth suppression in human NSCLC cell lines with IC30 values of 2.45-8.83 nM, with the exception of H157 with IC30 of >20 nM. Ridaforolimus treatment causes dephosphorylation of p70S6KThr389 in A549, H1703 and H157 cells, except H1666 that may express a resistant variant of mTORC1, and causes increased phosphorylation of pAKTser473 and pAKTThr308 in A549 and H1703 cells. Ridaforolimus, when combined with the MEK inhibitors CI-1040 or PD0325901, exhibits dose-dependent synergism in lung cancer cell lines, which is associated with the suppression of proliferation rather than enhancement of cell death, involving the inhibition of ribosomal biogenesis by 40% within 24 hours and a decreased polysome/monosome ratio.


References

Gadducci, A., et al.: Gynecol. Endocrinol., 24, 239 (2008), Gridelli, C., et al.: Oncol., 13, 139 (2008), Mita, M., et al.: J. Clin. Oncol., 26, 361 (2008), Hartford, C., et al.: Clin. Canc. Res., 15, 1428 (2009),

Appearance :
Crystalline powder
Physical State :
Solid
Solubility :
Soluble in DMSO
Storage :
Store at -20° C
Melting Point :
95-98° C
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
23724531
SMILES :
CC1CCC2CC(C(=CC=CC=CC(CC(C(=O)C(C(C(=CC(C(=O)CC(OC(=O)C3CCCCN3C(=O)C(=O)C1(O2)O)C(C)CC4CCC(C(C4)OC)OP(=O)(C)C)C)C)O)OC)C)C)C)OC

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Certificate of Analysis

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