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177262-30-5

177262-30-5 structure
177262-30-5 structure
  • Name: Didesmethylrocaglamide
  • Chemical Name: Didesmethylrocaglamide
  • CAS Number: 177262-30-5
  • Molecular Formula: C27H27NO7
  • Molecular Weight: 477.51
  • Catalog: Signaling Pathways Apoptosis Apoptosis
  • Create Date: 2020-08-09 10:08:20
  • Modify Date: 2024-01-10 22:54:29
  • 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].

Name Didesmethylrocaglamide
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].
Related Catalog
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.
References

[1]. Long-Sheng Chang, et al. Targeting Protein Translation by Rocaglamide and Didesmethylrocaglamide to Treat MPNST and Other Sarcomas. Mol Cancer Ther. 2020 Mar;19(3):731-741.

Molecular Formula C27H27NO7
Molecular Weight 477.51
Hazard Codes Xi