| Identification | Back Directory | [Name]
Zotatifin | [CAS]
2098191-53-6 | [Synonyms]
Zotatifin
Zotatifin (Synonyms: eFT226)
4-[(2S,3R,4S,5S,6R)-4-[(dimethylamino)methyl]-2,3-dihydroxy-10,12-dimethoxy-5-phenyl-7-oxa-11-azatricyclo[6.4.0.02,6]dodeca-1(12),8,10-trien-6-yl]benzonitrile
Benzonitrile, 4-[(5aR,6S,7S,8R,8aS)-7-[(dimethylamino)methyl]-6,7,8,8a-tetrahydro-8,8a-dihydroxy-1,3-dimethoxy-6-phenyl-5aH-cyclopenta[4,5]furo[3,2-c]pyridin-5a-yl]- | [Molecular Formula]
C28H29N3O5 | [MDL Number]
MFCD32874093 | [MOL File]
2098191-53-6.mol | [Molecular Weight]
487.55 |
| Chemical Properties | Back Directory | [Boiling point ]
622.4±55.0 °C(Predicted) | [density ]
1.36±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
10.10±0.70(Predicted) | [color ]
White to off-white | [InChIKey]
QYCXWOACFWMQFO-WZWZCULESA-N | [SMILES]
C(#N)C1=CC=C([C@]23[C@H](C4=CC=CC=C4)[C@@H](CN(C)C)[C@@H](O)[C@@]2(O)C2=C(O3)C=C(OC)N=C2OC)C=C1 |
| Hazard Information | Back Directory | [Uses]
Zotatifin (eFT226) is a potent, selective, and well-tolerated eIF4A inhibitor. Zotatifin promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs (IC50=2 nM) and interferes with the assembly of the eIF4F initiation complex[1]. Zotatifin shows robust antiviral effects, it effectively reduces viral infectivity by inhibiting SARS-CoV-2 NP protein biogenesis (IC90=37 nM)[2]. Zotatifin induces cell apoptosis[1]. | [in vivo]
Zotatifin (intravenous injection; 1 mg/kg; 14-22 days) decreases tumor volume, inhibits the TMD8 xenograft-bearing, HBL1 xenograft-bearing, Pfeiffer xenograft-bearing, SU-DHL-6 xenograft-bearing, SU-DHL-10 xenograft-bearing and Ramos-bearing animals’tumor growth as percentage of 97%, 87%, 70%, 83%, 37% and 75%, respectively[1].Zotatifin (intravenous injection; 0.001 mg/kg-1 mg/kg; 15 days) inhibits the growth of B-cell lymphoma xenografts and is well-tolerated against B-cell lymphoma xenograft models in vivo[1]. | Animal Model: | B-cell lymphoma xenograft model[1] | | Dosage: | 0.001 mg/kg; 0.1 mg/kg; 1 mg/kg | | Administration: | Intravenous injection; 15 days | | Result: | Showed efficacy in B-cell lymphoma xenograft models.
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| [IC 50]
eIF4 | [References]
[1] Peggy A. Thompson, et al. Preclinical Evaluation of eFT226, a Novel, Potent and Selective eIF4A Inhibitor with Anti-tumor Activity in B-cell Malignancies.
[2] Gordon DE, et al. A?SARS-CoV-2?protein?interaction?map?reveals?targets?for?drug?repurposing.Nature.?2020 Apr 30. DOI:10.1038/s41586-020-2286-9 |
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| Company Name: |
Wuhan Topule
|
| Telephone: |
+86-02787215551 19945035818 |
| Website: |
http://www.topule.com/ |
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