| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| References | |
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| Additional Infomation |
Zotatifin is being investigated in the clinical trial NCT04092673 (Eft226 in patients with specific advanced solid tumors). Zotatifin is a selective inhibitor of eukaryotic translation initiation factor 4A (eIF4A) with potential antitumor activity. After administration, Zotatifin targets and binds to eIF4A, promoting the binding of eIF4A to mRNAs containing specific polypurine motifs within the 5' untranslated region (5'-UTR), thereby forming a stable sequence-specific ternary complex (eIF4A-zotatifin-mRNA). This leads to the inhibition of translation of key oncogenes and anti-apoptotic proteins involved in tumor cell proliferation, survival, and metastasis, such as KRAS, Myc, myeloid leukemia-1 (Mcl-1), B-cell lymphoma-2 (Bcl-2), cyclin-dependent kinases (CDKs) 4 and 6, cyclin D, fibroblast growth factor receptor (FGFR) 1 and 2, human epidermal growth factor receptor 2 (HER2; ERBB2), and β-catenin. The inhibition of these oncogene expression results in the suppression of multiple oncogenic signaling pathways, thereby inhibiting tumor cell proliferation and inducing apoptosis. eIF4A is an RNA helicase and a rate-limiting component of the eukaryotic translation initiation complex. It catalyzes ATP-dependent RNA double-strand unwinding and promotes the scanning of 43S ribosomes within the 5' untranslated region (5'-UTR). eIF4A can be activated by multiple oncogenic signaling pathways, including the RAS/mitogen-activated protein kinase (MAPK) pathway and the phosphatidylinositol 3-kinase (PI3K)/AKT pathway, and regulates the translation of oncogenes and tumor survival factors with complex secondary structures in the 5'-UTR. These genes and factors are essential for the proliferation, survival and metastasis of tumor cells.
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| Molecular Formula |
C28H29N3O5
|
|---|---|
| Molecular Weight |
487.55
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| Exact Mass |
487.21
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| CAS # |
2098191-54-7
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| Related CAS # |
Zotatifin;2098191-53-6
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| PubChem CID |
129138801
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
2.4
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
36
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| Complexity |
819
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| Defined Atom Stereocenter Count |
5
|
| 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
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| InChi Key |
QYCXWOACFWMQFO-WZWZCULESA-N
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| InChi Code |
InChI=1S/C28H29N3O5/c1-31(2)16-20-23(18-8-6-5-7-9-18)28(19-12-10-17(15-29)11-13-19)27(33,25(20)32)24-21(36-28)14-22(34-3)30-26(24)35-4/h5-14,20,23,25,32-33H,16H2,1-4H3/t20-,23-,25-,27+,28+/m1/s1
|
| Chemical Name |
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
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~12.5 mg/mL (~25.6 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.56 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (12.5 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (2.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (12.5 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0511 mL | 10.2554 mL | 20.5107 mL | |
| 5 mM | 0.4102 mL | 2.0511 mL | 4.1021 mL | |
| 10 mM | 0.2051 mL | 1.0255 mL | 2.0511 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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