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| Targets |
TAR RNA-binding protein 2 (TRBP); Anticancer agent 73 potently targets TRBP and disrupts its interaction with Dicer. TRBP is a double-stranded RNA-binding protein that is a component of the RNA-induced silencing complex (RISC) and is involved in the microRNA (miRNA) biogenesis pathway. By disrupting the TRBP-Dicer interaction, the compound alters the processing of precursor miRNAs, leading to a rebalancing of oncogenic and tumor-suppressive miRNA expression. This results in the suppression of cancer cell proliferation and metastasis.
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| ln Vitro |
Anticancer agent 73 (compound CIB-3b) has been shown to increase E-cadherin expression and decrease protein expression levels of fibronectin, N-cadherin, and vimentin in SK-HEP-1 cells. Additionally, it has been observed to inhibit the biogenesis of miRNA, which in turn prevents SK-HEP-1, HCCLM3, and MHCC97L cells from proliferating and migrating [1].
In vitro, Anticancer agent 73 suppresses the proliferation and metastasis of HCC cells. It increases the expression of E-cadherin, an epithelial marker, and decreases the expression of mesenchymal markers, indicating a reversal of epithelial-mesenchymal transition (EMT). The compound modulates the expression profile of miRNAs and the proteome in HCC cells. It rebalances the expression of oncogenic and tumor-suppressive miRNAs. These effects contribute to its anticancer activity. |
| ln Vivo |
Anticancer agent 73 reduced the migration and proliferation of SK-HEP-1 and SK-HEP-1 implanted in SCID mice (10, 25, and 50 mg/kg; intravenously every two days for four weeks) [1].
In vivo, Anticancer agent 73 suppresses the growth and metastasis of HCC in animal models. The compound modulates the miRNA and protein expression profiles in tumors, leading to inhibition of tumor progression. It increases E-cadherin expression and decreases mesenchymal markers in vivo. The compound shows potential as a therapeutic agent for HCC by targeting the TRBP-Dicer interaction and rebalancing miRNA expression. |
| Enzyme Assay |
In vitro assays are performed using HCC cell lines. Cells are treated with Anticancer agent 73 at various concentrations for specified time periods. Cell proliferation, migration, and invasion are measured using standard assays such as MTT, wound healing, and transwell assays. The expression of E-cadherin and mesenchymal markers is assessed by Western blotting or immunocytochemistry. miRNA and protein expression profiles are analyzed using microarray or sequencing technologies. The compound is typically dissolved in DMSO for in vitro studies.
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| Animal Protocol |
In vivo efficacy is evaluated in xenograft or orthotopic mouse models of HCC. Anticancer agent 73 is administered to tumor-bearing mice, typically via intraperitoneal or oral routes. Tumor growth and metastasis are monitored over time. The expression of E-cadherin, mesenchymal markers, and miRNA/protein profiles are analyzed in tumor tissues. The compound's effects on tumor progression and metastasis are assessed. All procedures are conducted in accordance with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
Anticancer agent 73 has a molecular weight of 261.27 and the chemical formula C₁₄H₁₅NO₄. It is supplied as a solid powder. The compound is soluble in DMSO. Stability information, particularly in solution, has rarely been reported. It should be stored in a sealed container in a cool, dry place, protected from light. The compound is for research use only and not for human therapeutic use.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Anticancer agent 73 are not extensively documented. As an anticancer compound, it is expected to have cytotoxic effects on cancer cells. The compound is for research use only and not for human therapeutic use. It should be handled with appropriate safety precautions, including the use of personal protective equipment. The compound should be stored in a sealed container in a cool, dry place away from incompatible materials.
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| References | |
| Additional Infomation |
Anticancer agent 73 is also known as compound CIB-3b. It is an anticancer agent that targets TAR RNA-binding protein 2 (TRBP) and disrupts its interaction with Dicer. It rebalances the expression profile of oncogenic or tumor-suppressive miRNAs. It suppresses the proliferation and metastasis of HCC in vitro and in vivo. It increases E-cadherin expression and decreases mesenchymal markers. It is supplied as a solid powder and should be stored in a cool, dry place. It is for research use only.
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| Molecular Formula |
C14H15NO4
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| Molecular Weight |
261.2732
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| Exact Mass |
261.1
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| CAS # |
124811-87-6
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| PubChem CID |
20064063
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| Appearance |
White to light yellow solid powder
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| LogP |
2.835
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
19
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| Complexity |
302
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCOC(=O)C1=C(OC(=N1)C2=CC=C(C=C2)OC)C
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| InChi Key |
DAFRLXQGMZPMLA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H15NO4/c1-4-18-14(16)12-9(2)19-13(15-12)10-5-7-11(17-3)8-6-10/h5-8H,4H2,1-3H3
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| Chemical Name |
ethyl 2-(4-methoxyphenyl)-5-methyl-1,3-oxazole-4-carboxylate
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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 : ~100 mg/mL (~382.75 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.57 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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: ≥ 2.5 mg/mL (9.57 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8275 mL | 19.1373 mL | 38.2746 mL | |
| 5 mM | 0.7655 mL | 3.8275 mL | 7.6549 mL | |
| 10 mM | 0.3827 mL | 1.9137 mL | 3.8275 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.
Products are for research use only; We do not sell to patients
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