FLT3-IN-6
Based on 1 Customer Validation
FLT3-IN-6 is a potent and selective inhibitor of FLT3-ITD (FLT3 mutation) with an IC50 of 1.336 nM.
For research use only. We do not sell to patients.
- Purity: 99.25%
- CAS No.: 2377141-31-4
- Formula: C23H25N5O3
- Molecular Weight:419.48
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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
IC50: 1.336 nM (FLT3-ITD)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
0.107 μM
Compound: 46
|
Growth inhibition of mouse BAF3 cells transformed with FLT3 ITD mutant measured after 72 hrs by Celltiter-Glo assay
Growth inhibition of mouse BAF3 cells transformed with FLT3 ITD mutant measured after 72 hrs by Celltiter-Glo assay
|
[PMID: 31103903] |
| BaF3 | IC50 |
0.146 μM
Compound: 46
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Growth inhibition of mouse BAF3 cells transformed with FLT3 ITD/D835V double mutant measured after 72 hrs by Celltiter-Glo assay
Growth inhibition of mouse BAF3 cells transformed with FLT3 ITD/D835V double mutant measured after 72 hrs by Celltiter-Glo assay
|
[PMID: 31103903] |
| BaF3 | IC50 |
0.211 μM
Compound: 46
|
Growth inhibition of mouse BAF3 cells transformed with FLT3 D835V mutant measured after 72 hrs by Celltiter-Glo assay
Growth inhibition of mouse BAF3 cells transformed with FLT3 D835V mutant measured after 72 hrs by Celltiter-Glo assay
|
[PMID: 31103903] |
| BaF3 | IC50 |
0.532 μM
Compound: 46
|
Growth inhibition of mouse BAF3 cells transformed with FLT3 ITD/F691L double mutant measured after 72 hrs by Celltiter-Glo assay
Growth inhibition of mouse BAF3 cells transformed with FLT3 ITD/F691L double mutant measured after 72 hrs by Celltiter-Glo assay
|
[PMID: 31103903] |
| BaF3 | IC50 |
146 nM
Compound: LU-46
|
Antiproliferative activity against mouse BaF3 cells harboring FLT3-ITD-D835V mutant assessed as reduction in cell viability measured after 72 hrs by CellTiterGlo luminescent assay
Antiproliferative activity against mouse BaF3 cells harboring FLT3-ITD-D835V mutant assessed as reduction in cell viability measured after 72 hrs by CellTiterGlo luminescent assay
|
[PMID: 34550682] |
| BaF3 | IC50 |
532 nM
Compound: LU-46
|
Antiproliferative activity against mouse BaF3 cells harboring FLT3-ITD-F691L mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiterGlo luminescent assay
Antiproliferative activity against mouse BaF3 cells harboring FLT3-ITD-F691L mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiterGlo luminescent assay
|
[PMID: 34550682] |
| BaF3 | IC50 |
9.197 μM
Compound: 46
|
Growth inhibition of mouse BAF3 cells measured after 72 hrs by Celltiter-Glo assay
Growth inhibition of mouse BAF3 cells measured after 72 hrs by Celltiter-Glo assay
|
[PMID: 31103903] |
| MOLM-13 | IC50 |
33.2 nM
Compound: 46
|
Growth inhibition of human MOLM13 cells expressing FLT3 ITD mutant measured after 72 hrs by Celltiter-Glo assay
Growth inhibition of human MOLM13 cells expressing FLT3 ITD mutant measured after 72 hrs by Celltiter-Glo assay
|
[PMID: 31103903] |
| MV4-11 | IC50 |
27 nM
Compound: 46
|
Growth inhibition of human MV4-11 cells measured after 72 hrs by Celltiter-Glo assay
Growth inhibition of human MV4-11 cells measured after 72 hrs by Celltiter-Glo assay
|
[PMID: 31103903] |
| MV4-11 | IC50 |
27 nM
Compound: LU-46
|
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiterGlo luminescent assay
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiterGlo luminescent assay
|
[PMID: 34550682] |
| RPMI-8226 | IC50 |
3795 nM
Compound: 46
|
Growth inhibition of human RPMI8226 cells measured after 72 hrs by Celltiter-Glo assay
Growth inhibition of human RPMI8226 cells measured after 72 hrs by Celltiter-Glo assay
|
[PMID: 31103903] |
Chemical Information
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CAS No. 2377141-31-4
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Appearance Solid
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Molecular Weight 419.48
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Formula C23H25N5O3
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Color White to off-white
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SMILES
O=C(C1=CC=C(NC2CCN(C)CC2)C=C1)NC3=NNC(C4=CC=C(OCO5)C5=C4)=C3
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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 : 250 mg/mL (595.98 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 (4.96 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.96 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 (271 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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Handling Instructions (2659 KB)
References
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 | 2.3839 mL | 11.9195 mL | 23.8390 mL | 59.5976 mL |
| 5 mM | 0.4768 mL | 2.3839 mL | 4.7678 mL | 11.9195 mL | |
| 10 mM | 0.2384 mL | 1.1920 mL | 2.3839 mL | 5.9598 mL | |
| 15 mM | 0.1589 mL | 0.7946 mL | 1.5893 mL | 3.9732 mL | |
| 20 mM | 0.1192 mL | 0.5960 mL | 1.1920 mL | 2.9799 mL | |
| 25 mM | 0.0954 mL | 0.4768 mL | 0.9536 mL | 2.3839 mL | |
| 30 mM | 0.0795 mL | 0.3973 mL | 0.7946 mL | 1.9866 mL | |
| 40 mM | 0.0596 mL | 0.2980 mL | 0.5960 mL | 1.4899 mL | |
| 50 mM | 0.0477 mL | 0.2384 mL | 0.4768 mL | 1.1920 mL | |
| 60 mM | 0.0397 mL | 0.1987 mL | 0.3973 mL | 0.9933 mL | |
| 80 mM | 0.0298 mL | 0.1490 mL | 0.2980 mL | 0.7450 mL | |
| 100 mM | 0.0238 mL | 0.1192 mL | 0.2384 mL | 0.5960 mL |