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| Targets |
IMP2 (IGF2BP2). IMP2-IN-1 is an effective inhibitor of IMP2, targeting its RNA-binding function. IMP2 is involved in cancer progression through regulation of mRNA stability and translation. By inhibiting IMP2 RNA binding, IMP2-IN-1 reduces IMP2 protein levels in cancer cells and suppresses cell viability, particularly in colorectal (SW480) and liver (Huh7) cancer cell lines.
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| ln Vitro |
IMP2-IN-1 reduces IMP2 levels in SW480 colorectal cancer cells. It significantly reduces the viability of both differentiated and undifferentiated Huh7 hepatocellular carcinoma cells. The compound shows an IC50 of 81.3-127.5 microM for IMP2 RNA sequence binding, indicating its effectiveness in disrupting IMP2-mRNA interactions. Its activity is concentration-dependent.
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| ln Vivo |
No in vivo activity data for IMP2-IN-1 are provided in the reference sources. Based on its mechanism targeting IMP2, a key oncogenic RNA-binding protein, in vivo studies would likely involve subcutaneous xenograft models of liver or colorectal cancer, with daily oral or intraperitoneal administration.
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| Enzyme Assay |
Not explicitly detailed in reference sources. A typical IMP2 RNA-binding assay involves incubating recombinant IMP2 protein with a biotinylated RNA probe containing the IMP2 recognition sequence. IMP2-IN-1 at various concentrations is added, and IMP2-RNA binding is measured using streptavidin pull-down followed by Western blot or ELISA detection of bound IMP2.
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| Cell Assay |
SW480 cells are treated with IMP2-IN-1 at various concentrations, and cell lysates are analyzed by Western blot for IMP2 protein levels. For viability assays, Huh7 cells (differentiated and undifferentiated) are seeded in 96-well plates and treated with IMP2-IN-1 for 48-72 hours, and cell viability is measured using MTT or CellTiter-Glo assay.
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| Animal Protocol |
No in vivo animal experimental protocols for IMP2-IN-1 are provided in the reference sources. A typical in vivo study would use nude mice bearing SW480 or Huh7 xenograft tumors. After tumor establishment, mice would receive IMP2-IN-1 by oral gavage or intraperitoneal injection daily for 2-4 weeks, with tumor volume measurements every 2-3 days.
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| ADME/Pharmacokinetics |
Not explicitly detailed in reference sources. IMP2-IN-1 has a molecular weight of 401.34 and formula C21H14F3NO4. It is soluble in DMSO. Storage should be at -20degC as powder; in solution, it is stable at -80degC for 6 months or -20degC for 1 month. For in vivo formulation, various co-solvent systems may be used (e.g., 5% DMSO + 30% PEG300 + 5% Tween80 + 60% saline).
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| Toxicity/Toxicokinetics |
No toxicity data for IMP2-IN-1 are provided in the reference sources. As with all research compounds, standard safety precautions should be followed. The compound is for research use only and not intended for human use. Comprehensive toxicity studies would be required for any future clinical development.
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| References | |
| Additional Infomation |
IMP2-IN-1 is a research compound not yet approved for clinical use. It serves as a valuable tool for studying the role of IMP2 in cancer biology, particularly in liver and colorectal cancers. By inhibiting IMP2, an RNA-binding protein that promotes tumor progression, IMP2-IN-1 offers a novel approach to targeting cancer through the post-transcriptional regulation pathway.
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| Molecular Formula |
C21H14F3NO4
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|---|---|
| Molecular Weight |
401.34
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| Exact Mass |
401.087
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| CAS # |
1480482-51-6
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| PubChem CID |
72710917
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| Appearance |
White to off-white solid powder
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| LogP |
5.6
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
569
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)C2=CC=C(C=C2)C(=O)NC3=C(C=C(C=C3)OC(F)(F)F)C(=O)O
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| InChi Key |
ACJZUAUURQGKNK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H14F3NO4/c22-21(23,24)29-16-10-11-18(17(12-16)20(27)28)25-19(26)15-8-6-14(7-9-15)13-4-2-1-3-5-13/h1-12H,(H,25,26)(H,27,28)
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| Chemical Name |
2-[(4-phenylbenzoyl)amino]-5-(trifluoromethoxy)benzoic acid
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4917 mL | 12.4583 mL | 24.9165 mL | |
| 5 mM | 0.4983 mL | 2.4917 mL | 4.9833 mL | |
| 10 mM | 0.2492 mL | 1.2458 mL | 2.4917 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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