Deforolimus

CAS No. 572924-54-0

Deforolimus( AP-23573 | MK-8669 | Ridaforolimus )

Catalog No. M15090 CAS No. 572924-54-0

A potent, selective mTOR inhibitor with IC50 of 0.2 nM in HT-1080 cell line.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 46 In Stock
10MG 73 In Stock
25MG 149 In Stock
50MG 267 In Stock
100MG Get Quote In Stock
200MG Get Quote In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    Deforolimus
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, selective mTOR inhibitor with IC50 of 0.2 nM in HT-1080 cell line.
  • Description
    A potent, selective mTOR inhibitor with IC50 of 0.2 nM in HT-1080 cell line; displays significant antiproliferative activity a broad panel of cell lines with EC50 of 0.2-2.3 nM; potently and selectively inhibits VEGF production in a dose-dependent manner; exerts significant antitumor effects in mice bearing PC-3 (prostate), HCT-116 (colon), MCF7 (breast), PANC-1 (pancreas) or A549 (lung) xenografts.Breast Cancer Phase 2 Clinical(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.(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.
  • 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.
  • 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.
  • Synonyms
    AP-23573 | MK-8669 | Ridaforolimus
  • Pathway
    PI3K/Akt/mTOR signaling
  • Target
    mTOR
  • Recptor
    mTOR
  • Research Area
    Cancer
  • Indication
    Breast Cancer

Chemical Information

  • CAS Number
    572924-54-0
  • Formula Weight
    990.2061
  • Molecular Formula
    C53H84NO14P
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 44 mg/mL
  • 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 |r,c:31,50,t:46,48|
  • Chemical Name
    Rapamycin, 42-(dimethylphosphinate) (9CI)

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Rivera VM, et al. Mol Cancer Ther. 2011 Jun;10(6):1059-71. 2. Legrier ME, et al. Cancer Res. 2007 Dec 1;67(23):11300-8. 3. Becker MA, et al. BMC Cancer. 2016 Oct 20;16(1):814.
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