| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 2mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
Insulin-like growth factor 2 mRNA binding protein (IGF2BP1)[1]
AVJ16 targets the insulin-like growth factor 2 mRNA binding protein 1 (IGF2BP1). IGF2BP1 is an RNA-binding protein that regulates the translation of certain genes by binding to their mRNAs. By binding to IGF2BP1 with a Kd of 1.4 μM, AVJ16 interferes with its ability to bind target mRNAs, thereby modulating gene expression and protein translation. |
|---|---|
| ln Vitro |
In vitro, AVJ16 has been shown to inhibit the migration of H1299 cells that highly express endogenous IGF2BP1. Its activity is assessed using cell-based assays that measure cell migration, such as wound healing or transwell assays. These studies confirm its potential as a therapeutic agent for cancers where IGF2BP1 plays a role in metastasis.
|
| ln Vivo |
In vivo activity of AVJ16 is not extensively documented. As a cancer cell migration inhibitor, its efficacy would likely be evaluated in animal models of cancer metastasis. By inhibiting IGF2BP1, it may suppress tumor cell migration and invasion, thereby reducing metastatic spread. Further studies are needed to fully characterize its in vivo effects.
|
| Enzyme Assay |
Cell-free assays for AVJ16 typically involve measuring its binding affinity to IGF2BP1 using surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC). The Kd value of 1.4 μM is determined using these techniques. These assays are used to characterize the compound's potency and specificity for IGF2BP1.
|
| Cell Assay |
In vitro cellular assays are conducted to evaluate the functional activity of AVJ16. Cancer cell lines with high IGF2BP1 expression, such as H1299 cells, are treated with the compound. Cell migration is measured to assess the compound's effects on cell motility. The binding of IGF2BP1 to its target mRNAs is also assessed to confirm target engagement.
|
| Animal Protocol |
In vivo animal experiments typically involve xenograft models of cancer, particularly models that assess metastasis. Mice bearing tumors are administered AVJ16. Tumor growth and metastatic spread are monitored over time to assess the compound's efficacy. These studies are essential for demonstrating the in vivo activity of the compound.
|
| ADME/Pharmacokinetics |
The pharmacokinetic properties of AVJ16 are typical of a small molecule inhibitor. Its molecular weight is 469.53. While detailed PK parameters are not widely published, its properties suggest it is designed to have favorable drug-like characteristics, including good permeability and metabolic stability, to support efficacy in vivo.
|
| Toxicity/Toxicokinetics |
The toxicity profile of AVJ16 is not extensively documented but is likely to be similar to other small molecule inhibitors. Common adverse effects may include fatigue, gastrointestinal disturbances, and liver enzyme elevations. Preclinical studies would typically involve acute and chronic dosing in animal models to assess safety margins and identify potential target organ toxicities.
|
| References | |
| Additional Infomation |
AVJ16 is a research compound that targets IGF2BP1, an RNA-binding protein involved in cancer cell migration. It inhibits the migration of cancer cells that highly express IGF2BP1. The compound is used to study the role of IGF2BP1 in cancer metastasis and to develop potential therapeutic strategies. It is not approved for therapeutic use.
|
| Molecular Formula |
C28H27N3O4
|
|---|---|
| Molecular Weight |
469.531687021255
|
| Exact Mass |
469.2
|
| CAS # |
2775241-92-2
|
| PubChem CID |
163196422
|
| Appearance |
Off-white to light yellow solid powder
|
| LogP |
3.6
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
35
|
| Complexity |
721
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1CN(CCN1C2=CC3=C(C=C2)OCO3)C(=O)C4=CC=C(C=C4)CN5C6=CC=CC=C6C=C5CO
|
| InChi Key |
SBMDRXUGWAAAMV-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C28H27N3O4/c32-18-24-15-22-3-1-2-4-25(22)31(24)17-20-5-7-21(8-6-20)28(33)30-13-11-29(12-14-30)23-9-10-26-27(16-23)35-19-34-26/h1-10,15-16,32H,11-14,17-19H2
|
| Chemical Name |
[4-(1,3-benzodioxol-5-yl)piperazin-1-yl]-[4-[[2-(hydroxymethyl)indol-1-yl]methyl]phenyl]methanone
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: 250 mg/mL (532.45 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.43 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 20.8 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: ≥ 2.08 mg/mL (4.43 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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1298 mL | 10.6489 mL | 21.2979 mL | |
| 5 mM | 0.4260 mL | 2.1298 mL | 4.2596 mL | |
| 10 mM | 0.2130 mL | 1.0649 mL | 2.1298 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
Copyright 2020 InvivoChem LLC | All Rights Reserved
