FLT3/CHK1-IN-1
Based on 1 Customer Validation
FLT3/CHK-IN-1 (Compound 18) is a dual inhibitor of FLT3/CHK1. FLT3/CHK-IN-1 is more than 1700 times more selective to c-KI T and greatly reduces hERG affinity with an IC50 value of 58.4 μM. FLT3/CHK-IN-1 inhibits tumor growth in mouse xenotransplantation models inoculated with MV-4-11 cells.
For research use only. We do not sell to patients.
- Purity: 99.37%
- CAS No.: 2991054-23-8
- Formula: C25H33F3N6O2
- Molecular Weight:506.56
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
8.2 nM
Compound: 18
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Antiproliferative activity against mouse BaF3 cells harboring FLT3-ITD-N701K mutation assessed as reduction in cell viability incubated for 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay
Antiproliferative activity against mouse BaF3 cells harboring FLT3-ITD-N701K mutation assessed as reduction in cell viability incubated for 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay
|
[PMID: 37584545] |
| JeKo-1 | IC50 |
260 nM
Compound: 18
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Antiproliferative activity against human JeKo-1 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay
Antiproliferative activity against human JeKo-1 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay
|
[PMID: 37584545] |
| MV4-11 | IC50 |
0.21 nM
Compound: 18
|
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay
|
[PMID: 37584545] |
| Z-138 | IC50 |
115 nM
Compound: 18
|
Antiproliferative activity against human Z138 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay
Antiproliferative activity against human Z138 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay
|
[PMID: 37584545] |
Chemical Information
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CAS No. 2991054-23-8
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Appearance Solid
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Molecular Weight 506.56
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Formula C25H33F3N6O2
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Color White to off-white
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SMILES
N[C@H]1CC[C@@H](NC2=NC(NC3=CC4=C(C=C3)CN(C(CC(O)(C)C)=O)CC4)=NC=C2C(F)(F)F)CC1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL (197.41 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 (protect from light). 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 (protect from light). 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: 2.5 mg/mL (4.94 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.94 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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 (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 (protect from light). 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 | 1.9741 mL | 9.8705 mL | 19.7410 mL | 49.3525 mL |
| 5 mM | 0.3948 mL | 1.9741 mL | 3.9482 mL | 9.8705 mL | |
| 10 mM | 0.1974 mL | 0.9870 mL | 1.9741 mL | 4.9352 mL | |
| 15 mM | 0.1316 mL | 0.6580 mL | 1.3161 mL | 3.2902 mL | |
| 20 mM | 0.0987 mL | 0.4935 mL | 0.9870 mL | 2.4676 mL | |
| 25 mM | 0.0790 mL | 0.3948 mL | 0.7896 mL | 1.9741 mL | |
| 30 mM | 0.0658 mL | 0.3290 mL | 0.6580 mL | 1.6451 mL | |
| 40 mM | 0.0494 mL | 0.2468 mL | 0.4935 mL | 1.2338 mL | |
| 50 mM | 0.0395 mL | 0.1974 mL | 0.3948 mL | 0.9870 mL | |
| 60 mM | 0.0329 mL | 0.1645 mL | 0.3290 mL | 0.8225 mL | |
| 80 mM | 0.0247 mL | 0.1234 mL | 0.2468 mL | 0.6169 mL | |
| 100 mM | 0.0197 mL | 0.0987 mL | 0.1974 mL | 0.4935 mL |