I3IN-002
Based on 1 Customer Validation
I3IN-002 is a small-molecule RNA-binding protein IGF2BP3 inhibitor with an IC50 value of approximately 2 μM in SEM cells. I3IN-002 interferes with interaction with m6 A-modified mRNAs, disrupting the stabilization of target genes (such as CDK6, MYC, and BCL2) to inhibit leukemic cell growth, induce cell cycle arrest, and promote apoptosis. I3IN-002 is promising for research of B-cell acute lymphoblastic leukemia.
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- Pureza: 99.35%
- No. CAS: 552829-57-9
- Fòrmula: C20H16F3N5OS
- Peso molecular:431.43
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
I3IN-002 (0.0001-100 μM) inhibits cell growth in SEM and Lin-MLL-Af4 cells, with IC50 values of 3.5 μM (SEM) and 10.1 μM (Lin-MLL-Af4 cells)[1].
I3IN-002 (5 μM) reduces extracellular acidification rate (ECAR) and lactate efflux rate in SEM cells[1].
I3IN-002 (5 μM) reduces m6A RNA modification levels in SEM cells[1].
I3IN-002 (2.5-10 μM, 4 days) induces cell cycle arrest in the Sub-G0 phase and promotes apoptosis in SEM and RS4;11 cells[2].
I3IN-002 (5-10 μM) reduces the plating efficiency of MLL-Af4 Lin- leukemic cells in methylcellulose colony formation assays in a dose-dependent manner, and decreases the proportion of CD34+c-kit+ leukemic initiating cells[2].
I3IN-002 (5 μM, 6 h) disrupts the binding of IGF2BP3 to target mRNAs (CDK6, MYC, BCL2, HOXA9) in SEM cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SEM and RS4;11 cells
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Concentration:5, 10 μM
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Incubation Time:4 days
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Result:Induced cell cycle arrest in the Sub-G0 phase.
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Cell Line:SEM and RS4;11 cells
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Concentration:2.5, 5, 10 μM
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Incubation Time:4 days
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Result:Promoted apoptosis in SEM and RS4;11 cells.
Increased Caspase 3/7 activity.
I3IN-002 (25 mg/kg, i.p., 3 times/week for 3 weeks) exhibits potent anti-leukemic efficacy in C57BL/6J, B6.SJL-Ptprca Pepcb/BoyJ (B6 CD45.1), and B6J.129(Cg)Gt(ROSA)26Sortm1.1Fezh/J (Cas9-GFP, BL/6J) mice with syngeneic MLL-Af4 leukemia transplantation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Lin-MLL-Af4 murine bone marrow cells were transplanted into C57BL/6J mice or Human B-ALL cells were engrafted into 6-10-week-old female NSG mice[1]
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Dosage:25 mg/kg
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Administration:i.p., three times a week, 3 weeks
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Result:Reduced m6A RNA modification levels in splenic tumors.
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Animal Model:Lin--MLL-Af4 murine leukemic cells (wild-type or IGF2BP3-knockout) were transplanted into busulfan-conditioned C57BL/6J, B6.SJL-Ptprca Pepcb/BoyJ (B6 CD45.1), or B6J.129(Cg)Gt(ROSA)26Sortm1.1 Fezh/J (Cas9-GFP, BL/6J) mice[2]
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Dosage:25 mg/kg
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Administration:i.p., three times a week, 3 weeks
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Result:Exhibited potent anti-leukemic efficacy.
Reduced spleen size and weight.
Decreased leukemic cell engraftment in liver, spleen, lung and kidney.
Improved overall survival of leukemic mice.
Reduced the number of CD34+c-kit+ leukemic initiating cells in the spleen and bone marrow.
Decreased the proportion of CD11b+ cells and CD34+Sca1- cells.
Chemical Information
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No. CAS 552829-57-9
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Appearance Solid
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Peso molecular 431.43
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Fòrmula C20H16F3N5OS
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Color Off-white to light yellow
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SMILES
O=C(NC1=C(C(F)(F)F)C=CC=C1)CSC(N=N2)=NC3=C2C4=CC(CC)=CC=C4N3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 20 mg/mL (46.36 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2 mg/mL (4.64 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3179 mL | 11.5894 mL | 23.1787 mL | 57.9468 mL |
| 5 mM | 0.4636 mL | 2.3179 mL | 4.6357 mL | 11.5894 mL | |
| 10 mM | 0.2318 mL | 1.1589 mL | 2.3179 mL | 5.7947 mL | |
| 15 mM | 0.1545 mL | 0.7726 mL | 1.5452 mL | 3.8631 mL | |
| 20 mM | 0.1159 mL | 0.5795 mL | 1.1589 mL | 2.8973 mL | |
| 25 mM | 0.0927 mL | 0.4636 mL | 0.9271 mL | 2.3179 mL | |
| 30 mM | 0.0773 mL | 0.3863 mL | 0.7726 mL | 1.9316 mL | |
| 40 mM | 0.0579 mL | 0.2897 mL | 0.5795 mL | 1.4487 mL |
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