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| Targets |
IMP1; c-Myc; NF-κB
INVIVO6620 specifically targets the interaction between IMP1 (IGF2BP1), an RNA-binding protein, and its target mRNA, c-Myc. IMP1 binds to the coding region instability determinant (CRD) of c-Myc mRNA, stabilizing it and promoting its translation. By inhibiting this binding, INVIVO6620 reduces the stability and translation of c-Myc mRNA, thereby decreasing c-Myc protein levels. This mechanism is relevant for studying cancer, as c-Myc is a key oncogene. |
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| ln Vitro |
Proteins encoded by target mRNAs are expressed more when the oncoembryonic mRNA binding protein IMP1 binds and stabilizes c-Myc, β-TrCP1, and other protein mRNAs [1]. In SK-MEL2 cells, BTYNB (10 μM; 0.5-1 hour) increases c-Myc mRNA and, in a dose-dependent manner, BTYNB (10-40 μM; 72 hours) lowers c-Myc expression [1]. 72-hour BTYNB (10–40 μM). In the presence of hormones, BTYNB (1-40 μM; 72 h) decreases CDC34, CALM1, β-TRCP1 and h) in T47D/(A1-2) cells and dose-dependently lowers IMP1 expression in SK-MEL2 cells [1]. The rapid proliferation of IMP1 cells is strongly inhibited by BTYNB, with IC50 values of 2.3 μM, 3.6 μM, and 4.5 μM in ES-2, IGROV-1, and SK-MEL2 cells, respectively. BTYNB did not suppress cell proliferation at any tested concentration, even 50 μM, and it had no effect on IMP1-negative cells [1].
In vitro, INVIVO6620 demonstrates potent and specific inhibition of IMP1 binding to c-Myc mRNA, with an IC50 of 5 μM. It displays selectivity and efficacy against IMP1-positive cancer/tumor cell lines. This suggests that it can specifically target cancer cells that rely on IMP1 for c-Myc expression, making it a valuable tool for studying the role of this interaction in tumor biology. |
| ln Vivo |
In vivo, INVIVO6620 is used in cancer research to study the effects of inhibiting the IMP1-c-Myc interaction. While specific in vivo efficacy data are not detailed in the provided sources, its mechanism of reducing c-Myc expression supports its potential for studying tumor growth inhibition. It is a valuable tool for validating IMP1 as a therapeutic target in cancer.
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| Enzyme Assay |
In vitro enzyme/receptor binding studies are not applicable to INVIVO6620, as its target is a protein-RNA interaction, not an enzyme or a receptor. Its activity is assessed using biochemical assays that measure the binding of IMP1 to c-Myc mRNA. For example, an RNA pull-down or a fluorescence polarization assay could be used in the presence of the inhibitor to determine its IC50 of 5 μM.
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| Cell Assay |
RT-PCR[1]
Cell Types: T47D/(A1-2) Cell Tested Concentrations: 1μM; 10μM; 20μM; 30μM; 40 μM Incubation Duration: Experimental Results: diminished levels of multiple cancer-related IMP1 mRNA targets. In vitro cellular assays for INVIVO6620 are used to study its effects on cancer cells. Cells are treated with the compound, and key readouts include the levels of c-Myc mRNA and protein, which are measured by qRT-PCR and Western blotting, respectively. Additionally, the effects on cell proliferation and viability are assessed. These assays confirm the compound's mechanism of action and its potential as an anticancer agent. |
| Animal Protocol |
In vivo animal studies for INVIVO6620 are not extensively detailed in the provided sources. However, as a tool for studying IMP1 biology, it would be used in xenograft models using IMP1-positive cancer cell lines. Tumor-bearing mice would be treated with the compound, and endpoints would include tumor growth inhibition and analysis of c-Myc expression in the tumor tissue.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of INVIVO6620 are indicated by its molecular weight of 309.18 g/mol and a molecular formula of C₁₂H₉BrN₂OS. It is a solid powder. Its solubility and other PK parameters are not detailed in the provided sources. For storage, it is typically kept at -20°C to maintain stability. These properties are important for its formulation and use in laboratory studies.
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| Toxicity/Toxicokinetics |
Toxicological data for INVIVO6620 are limited, as it is a research compound. Its primary value is as a tool for studying RNA biology and cancer. While specific toxicity profiles are not detailed, its mechanism of modulating c-Myc expression could have significant biological effects. Comprehensive safety studies are not available in the public domain.
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| References | |
| Additional Infomation |
INVIVO6620 is a research-use-only compound that acts as a potent and specific inhibitor of the IMP1-c-Myc mRNA interaction. Its CAS number is 304456-62-0. It is also known as BTYNB. This compound is a valuable tool for researchers studying the role of RNA-binding proteins in cancer. It is not an approved drug.
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| Molecular Formula |
C12H9BRN2OS
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|---|---|
| Molecular Weight |
309.181
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| Exact Mass |
307.961
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| Elemental Analysis |
C, 46.62; H, 2.93; Br, 25.84; N, 9.06; O, 5.17; S, 10.37
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| CAS # |
304456-62-0
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| Related CAS # |
304456-62-0
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| PubChem CID |
721984
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| Appearance |
White to light yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
495.9±40.0 °C at 760 mmHg
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| Flash Point |
253.7±27.3 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.685
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| LogP |
2.88
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
17
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| Complexity |
311
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(/N=C/C2=CC=C(S2)Br)C=CC=CC=1C(=O)N
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| InChi Key |
OZEADOPONHLEDS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H9BrN2OS/c13-11-6-5-8(17-11)7-15-10-4-2-1-3-9(10)12(14)16/h1-7H,(H2,14,16)
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| Chemical Name |
2-[(5-bromothiophen-2-yl)methylideneamino]benzamide
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| Synonyms |
BTYNB IMP1 Inhibitor
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: ~62 mg/mL (~200.5 mM)
Ethanol: ~4 mg/mL (~12.9 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.09 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 (8.09 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 (8.09 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 | 3.2344 mL | 16.1718 mL | 32.3436 mL | |
| 5 mM | 0.6469 mL | 3.2344 mL | 6.4687 mL | |
| 10 mM | 0.3234 mL | 1.6172 mL | 3.2344 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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