5'-Fluoroindirubinoxime
Based on 1 Customer Validation
5'-Fluoroindirubinoxime (5’-FIO, compound 13), an Indirubin (HY-N0117) derivative, is a potent FLT3 inhibitor, with an IC50 of 15 nM.
For research use only. We do not sell to patients.
- Purity: 98.0%
- CAS No.: 861214-33-7
- Formula: C16H10FN3O2
- Molecular Weight:295.27
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
15 nM (FLT3)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
12.2 μM
Compound: 25
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Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 24 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 24 hrs by MTT assay
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[PMID: 34161865] |
| HepG2 | IC50 |
10 μM
Compound: 15b
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Cytotoxicity against human HepG2 cells assessed as cell growth inhibition after 24 hrs by alamar blue assay
Cytotoxicity against human HepG2 cells assessed as cell growth inhibition after 24 hrs by alamar blue assay
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[PMID: 28743492] |
| HT-1080 | IC50 |
3.4 μM
Compound: 25
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Antiproliferative activity against human HT-1080 cells assessed as cell growth inhibition measured after 24 hrs by MTT assay
Antiproliferative activity against human HT-1080 cells assessed as cell growth inhibition measured after 24 hrs by MTT assay
|
[PMID: 34161865] |
| MV4-11 | IC50 |
0.072 μM
Compound: 13
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Antiproliferative activity against wild type FLT3 expressing human MV411 cells after 72 hrs by WST8 assay
Antiproliferative activity against wild type FLT3 expressing human MV411 cells after 72 hrs by WST8 assay
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[PMID: 20153646] |
| RS4-11 | IC50 |
2.21 μM
Compound: 13
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Antiproliferative activity against human RS4:11 cells having FLT3-ITD mutation after 72 hrs by WST8 assay
Antiproliferative activity against human RS4:11 cells having FLT3-ITD mutation after 72 hrs by WST8 assay
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[PMID: 20153646] |
| SNU-638 | IC50 |
2.1 μM
Compound: 25
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Antiproliferative activity against human SNU-638 cells assessed as cell growth inhibition measured after 24 hrs by MTT assay
Antiproliferative activity against human SNU-638 cells assessed as cell growth inhibition measured after 24 hrs by MTT assay
|
[PMID: 34161865] |
5'-Fluoroindirubinoxime (5’-FIO, compound 13) exhibits IC50 values of 1.53 μM and 1.27 μM for VEGFR2 and Aurora A, respectively[1].
5'-Fluoroindirubinoxime (5’-FIO) exhibits IC50 values of 12.2 μM, 2.1 μM, 3.4 μM and 5.1 μM in A549, SNU-638, HT-1080 and RK3E-ras cancer cells, respectively. 5'-Fluoroindirubinoxime (5’-FIO) induces the apoptosis in RK3E-ras cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rat tumor model based RK3E-ras cells[2].
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Dosage:S.C..
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Administration:10 μmol/L/100 μL (~2.95 mg/mL) every other day beginning on day 6.
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Result:Effectively inhibited tumor growth.
Chemical Information
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CAS No. 861214-33-7
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Appearance Solid
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Molecular Weight 295.27
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Formula C16H10FN3O2
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Color Light brown to black
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SMILES
O=C1NC2=C(C=C(F)C=C2)/C1=C3NC4=C(C=CC=C4)C\3=N/O
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Synonyms
5'-FIO
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 83.33 mg/mL (282.22 mM; Need ultrasonic; 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: ≥ 2.08 mg/mL (7.04 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Choi SJ, et al. Indirubin derivatives as potent FLT3 inhibitors with anti-proliferative activity of acute myeloid leukemic cells. Bioorg Med Chem Lett. 2010 Mar 15;20(6):2033-7. [Content Brief]
[2]. Kim SA, et al. Antitumor activity of novel indirubin derivatives in rat tumor model. Clin Cancer Res. 2007 Jan 1;13(1):253-9. [Content Brief]
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 | 3.3867 mL | 16.9337 mL | 33.8673 mL | 84.6683 mL |
| 5 mM | 0.6773 mL | 3.3867 mL | 6.7735 mL | 16.9337 mL | |
| 10 mM | 0.3387 mL | 1.6934 mL | 3.3867 mL | 8.4668 mL | |
| 15 mM | 0.2258 mL | 1.1289 mL | 2.2578 mL | 5.6446 mL | |
| 20 mM | 0.1693 mL | 0.8467 mL | 1.6934 mL | 4.2334 mL | |
| 25 mM | 0.1355 mL | 0.6773 mL | 1.3547 mL | 3.3867 mL | |
| 30 mM | 0.1129 mL | 0.5645 mL | 1.1289 mL | 2.8223 mL | |
| 40 mM | 0.0847 mL | 0.4233 mL | 0.8467 mL | 2.1167 mL | |
| 50 mM | 0.0677 mL | 0.3387 mL | 0.6773 mL | 1.6934 mL | |
| 60 mM | 0.0564 mL | 0.2822 mL | 0.5645 mL | 1.4111 mL | |
| 80 mM | 0.0423 mL | 0.2117 mL | 0.4233 mL | 1.0584 mL | |
| 100 mM | 0.0339 mL | 0.1693 mL | 0.3387 mL | 0.8467 mL |