| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
IC50: 1.336 nM (FLT3-ITD)[1]
FLT3-ITD mutant (FLT3 with Internal Tandem Duplication mutations). FLT3-IN-6 is a selective inhibitor of FLT3-ITD, with an IC50 of 1.336 nM, and is designed to target the mutant form of FLT3 that is common in AML. |
|---|---|
| ln Vitro |
FLT3-IN-6 is a potent and selective inhibitor of FLT3-ITD with an IC50 of 1.336 nM. It effectively inhibits the mutated form of FLT3, which is a key driver in approximately 25-30% of AML patients. Its selectivity for the mutant form makes it a valuable tool in hematological malignancy research.
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| ln Vivo |
No specific in vivo activity data are reported for FLT3-IN-6. As a potent FLT3-ITD inhibitor, it is expected to have anti-tumor activity in AML xenograft models driven by FLT3-ITD mutations. It is valuable for studying FLT3-dependent signaling pathways and potential therapeutic interventions for FLT3-mutant AML.
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| Enzyme Assay |
Cell-free FLT3-ITD kinase assays are performed using recombinant FLT3-ITD enzyme. The compound is incubated with the enzyme and a peptide substrate in the presence of ATP for 30-60 minutes. Kinase activity is measured using a luminescence-based ADP detection kit or by 33P incorporation. IC50 (1.336 nM) is determined from a dose-response curve.
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| Cell Assay |
FLT3-ITD-positive human leukemia cell lines (e.g., MV4-11) are seeded in 96-well plates and treated with increasing concentrations of FLT3-IN-6 for 72 hours. Cell viability is assessed using the MTT assay or CellTiter-Glo reagent. Apoptosis is measured by Annexin V/PI staining. FLT3 phosphorylation and downstream signaling (p-STAT5, p-ERK) are assessed by Western blot.
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| Animal Protocol |
For in vivo studies, FLT3-IN-6 would be administered orally to mice bearing FLT3-ITD-driven tumor xenografts (e.g., MV4-11). Dosing is typically once or twice daily for 2-4 weeks. Tumor volumes are measured with calipers. At study termination, tumors are excised for pharmacodynamic analysis of FLT3 phosphorylation and downstream signaling. No published studies are available.
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| ADME/Pharmacokinetics |
No specific PK data are reported for FLT3-IN-6. The molecular weight is 405.45 (C21H23N7O3). CAS 2377141-31-4. It is soluble in DMSO (10-50 mg/mL). For in vivo studies, it would typically be formulated in 0.5% methylcellulose. Oral bioavailability and half-life have not been characterized. This compound is a research chemical.
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| Toxicity/Toxicokinetics |
No specific toxicity data are reported for FLT3-IN-6. As a FLT3-ITD inhibitor, potential on-target toxicity may include myelosuppression, as FLT3 plays a role in normal hematopoiesis. Comprehensive toxicological assessments have not been published. The compound is for research use only and is not an FDA-approved drug.
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| References | |
| Additional Infomation |
Other information: FLT3-IN-6 (CAS 2377141-31-4) is a research compound and not FDA-approved. It is a potent and selective inhibitor of FLT3-ITD with an IC50 of 1.336 nM. It is a valuable tool for studying FLT3-ITD-driven acute myeloid leukemia (AML). Purity ≥98%. For research use only.
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| Molecular Formula |
C23H25N5O3
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|---|---|
| Molecular Weight |
419.48
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| Exact Mass |
419.195
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| CAS # |
2377141-31-4
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| PubChem CID |
138454787
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
603.1±55.0 °C at 760 mmHg
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| Flash Point |
318.6±31.5 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.691
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| LogP |
3.35
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
31
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| Complexity |
606
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1CCC(CC1)NC2=CC=C(C=C2)C(=O)NC3=NNC(=C3)C4=CC5=C(C=C4)OCO5
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| InChi Key |
OKFAZZUSWJWRJN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H25N5O3/c1-28-10-8-18(9-11-28)24-17-5-2-15(3-6-17)23(29)25-22-13-19(26-27-22)16-4-7-20-21(12-16)31-14-30-20/h2-7,12-13,18,24H,8-11,14H2,1H3,(H2,25,26,27,29)
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| Chemical Name |
N-[5-(1,3-benzodioxol-5-yl)-1H-pyrazol-3-yl]-4-[(1-methylpiperidin-4-yl)amino]benzamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 250 mg/mL (595.98 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.96 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 (4.96 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.96 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3839 mL | 11.9195 mL | 23.8390 mL | |
| 5 mM | 0.4768 mL | 2.3839 mL | 4.7678 mL | |
| 10 mM | 0.2384 mL | 1.1920 mL | 2.3839 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.
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