Ridaforolimus

SKU: orb1300859

Description

Ridaforolimus

Research Area

Cell Biology, Infectious Disease & Virology, Signal Transduction

Key Properties

• CAS Number: 572924-54-0
• MW: 990.21
• Purity: 90.00%
• Formula: C₅₃H₈₄NO₁₄P
• SMILES: [H][C@@]12CC[C@@H](C)[C@@](O)(O1)C(=O)C(=O)N1CCCC[C@@]1([H])C(=O)O[C@@]([H])(CC(=O)[C@H](C)\C=C(C)\[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)\C=C\C=C\C=C(C)\[C@H](C2)OC)[C@H](C)C[C@@H]1CC[C@@H](OP(C)(C)=O)[C@@H](C1)OC
• Target: Antibacterial,Autophagy,mTOR
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:182 mg/mL (183.8 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (4.04 mM)

Bioactivity

• Target IC50:
  mTOR (HT-1080 cells):0.2 nM
• In Vivo:
  Deforolimus exhibits dose-dependent Inhibition of S6 and 4E-BP1 phosphorylation in HT-1080 cells, with IC50 Values of 0.2 nM and 5.6 nM, respectively and EC50 Values of 0.2 nM and 1.0 nM, respectively It leads to a reduction in cell size, an increase in G1 phase cells, and Inhibition of glucose uptake, with an EC50 range of 0.1-1 nM. Demonstrating significant ant Proliferative activity across a spectrum of cell lines, Deforolimus has EC50 Values ranging from 0.2 to 2.3 nM. It effectively and selectively inhibits VEGF production in a dose-dependent manner, with an EC50 of ~0.1 nM. When combined with MEK inhibitors CI-1040 or PD0325901 on human lung cancer cell lines, Deforolimus synergizes, leading to a dose-dependent reduction in cell proliferation rather than an increase in cell apoptosis. This combination, after a 24 hour treatment, results in a 40% Inhibition of ribosomal synthesis and a decrease in the ratio of polysomes to monosomes. Notably, Deforolimus significantly inhibit the growth of human NSCLC cell lines (except for H157 cells) with IC30 Values between 2.45-8.83 nM, but its effect on H157 cells shows an IC30 >20 nM. Treating A549, H1703, and H157 cells (excluding H1666 cells with mTORC1-resistant mutations) with 2.8-5.9 nM Deforolimus results in dephosphorylation of p70S6KThr389 and increased phosphorylation levels of pAKTser473 and pAKTThr308 in A549 and H1703 cells.
• In Vitro:
  Deforolimus exhibits significant antitumor activity in a dose-dependent manner in mice bearing xenografts of PC-3 (prostate), HCT-116 (colon), MCF7 (breast), PANC-1 (pancreas), or A549 (lung) cancers. It inhibit the mTOR signaling pathway in the SK-LMS-1 xenograft model associated wit the Inhibition of tumor growth.
• Cell Research:
  Cell lines: Colo205 h1755 h1395 h1666,A549,H157 and H1703 cells. concentration : Dissolved in ethanol final concentration ~ 1 μM. Method: Cells are seeded at 2-3 × 04 mL and serial dilutions of Deforolimus are added after 2 hours,for at least three cell doublings (72-120 hours).Deforolimus effects are measured b the CellTiter 96 Aqueous nonradioactive cell proliferation assay and Sulforhodamine B assays.
• Animal Research:
  Animal Models: Male and f Male athymic NCr-nu mice with xenografts established by subcutaneous implantation of PC-3,A549,HCT-116,MCF7,PANC-1 and SK-LMS-1 tumors. Formulation: Dissolved in ethanol and diluted in a Vehicle of 4% ethanol,5% Tween 80 and 5% propylene glycol. Dosages: ~10 mg/kg. Administration: Intraperitoneally injection

Storage & Handling

• Storage: Powder: -20°C for 3 years | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Ridaforolimus, MK8669, MK-8669, MK 8669, inhibit, mTOR, Mammalian target of Rapamycin, Inhibitor, AP 23573, AP23573, AP-23573, Autophagy, Deforolimus

Compound Identifiers

PubChem CID

11520894