1. Cell Cycle/DNA Damage
    Apoptosis
  2. Eukaryotic Initiation Factor (eIF)
    Apoptosis
  3. Didesmethylrocaglamide

Didesmethylrocaglamide 

Cat. No.: HY-19356A Purity: 98.40% ee.: 98.30%
Handling Instructions

Didesmethylrocaglamide, a derivative of Rocaglamide, is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. Didesmethylrocaglamide has potent growth-inhibitory activity with an IC50 of 5 nM. Didesmethylrocaglamide suppresses multiple growth-promoting signaling pathways and induces apoptosis in tumor cells. Antitumor activity.

For research use only. We do not sell to patients.

Didesmethylrocaglamide Chemical Structure

Didesmethylrocaglamide Chemical Structure

CAS No. : 177262-30-5

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Based on 1 publication(s) in Google Scholar

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Description

Didesmethylrocaglamide, a derivative of Rocaglamide, is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. Didesmethylrocaglamide has potent growth-inhibitory activity with an IC50 of 5 nM. Didesmethylrocaglamide suppresses multiple growth-promoting signaling pathways and induces apoptosis in tumor cells. Antitumor activity[1].

IC50 & Target

Eukaryotic initiation factor 4A (eIF4A)[1]

In Vitro

Didesmethylrocaglamide (5 nM, and 10 nM; 72 hours; MPNST cells) treatment arrests MPNST cells at G2-M, increases the sub-G1 population, induces cleavage of caspases and PARP, and elevates the levels of the DNA-damage response marker γH2A.X, while decreasing the expression of AKT and ERK1/2[1].
Didesmethylrocaglamide inhibits MPNST cell proliferation by inducing cell cycle arrest at G2/M and subsequently, cell death. Didesmethylrocaglamide-treated 697-R cells exhibits IC50 values is very similar to those of parental 697 cells (4 vs 3nM of IC50, respectively)[1].
Didesmethylrocaglamide induces apoptosis in both neurofibromatosis type 1 (NF1)-expressing and NF1-deficient MPNST cells, possibly subsequent to the activation of the DNA damage response. Didesmethylrocaglamide-treated sarcoma cells show decreased levels of multiple oncogenic kinases, including insulin-like growth factor-1 receptor[1].

Western Blot Analysis[1]

Cell Line: Malignant peripheral nerve sheath tumors (MPNST) cells
Concentration: 5 nM, and 10 nM
Incubation Time: 72 hours
Result: Induced cleavage of caspases and PARP, and elevated the levels of the DNA-damage response marker γH2A.X.
Molecular Weight

477.51

Formula

C₂₇H₂₇NO₇

CAS No.

177262-30-5

SMILES

O=C([[email protected]]([[email protected]]1C2=CC=CC=C2)[[email protected]@H](O)[[email protected]]3(O)[[email protected]@]1(C4=CC=C(OC)C=C4)OC5=CC(OC)=CC(OC)=C35)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (209.42 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0942 mL 10.4710 mL 20.9420 mL
5 mM 0.4188 mL 2.0942 mL 4.1884 mL
10 mM 0.2094 mL 1.0471 mL 2.0942 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

DidesmethylrocaglamideEukaryotic Initiation Factor (eIF)ApoptosiseIF4ASilvestrolRocaglamidederivativeantitumorgrowth-inhibitoryanti-proliferationPARPAKTERK1/2Inhibitorinhibitorinhibit

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Didesmethylrocaglamide
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HY-19356A
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