| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
FLT3[1]
FLT3-IN-10 targets FMS-like tyrosine kinase 3 (FLT3), a receptor tyrosine kinase frequently mutated or overexpressed in acute myeloid leukemia (AML). By binding to and inhibiting FLT3 kinase activity, it blocks downstream signaling pathways that promote the proliferation and survival of leukemic cells. This makes it a promising therapeutic strategy for FLT3-mutated AML. |
|---|---|
| ln Vitro |
In vitro, FLT3-IN-10 has been shown to be a potent inhibitor of FLT3 kinase activity. While specific IC50 values are not widely published, its activity is typically assessed using biochemical kinase assays that measure the phosphorylation of a substrate in the presence of the compound. These studies confirm its potential as a therapeutic agent for FLT3-mutated AML.
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| ln Vivo |
In vivo activity of FLT3-IN-10 has been studied in animal models of FLT3-mutated AML. Its efficacy is evaluated in xenograft models bearing FLT3-mutant tumors. By inhibiting FLT3 signaling, the compound is expected to suppress tumor growth and improve survival in these models. These studies are crucial for validating its therapeutic potential.
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| Enzyme Assay |
Cell-free assays for FLT3-IN-10 typically involve measuring its inhibitory activity against FLT3 kinase using biochemical kinase assays. The compound's IC50 value is determined by measuring the phosphorylation of a peptide substrate in the presence of varying concentrations of the inhibitor. These assays are used to characterize the compound's potency and selectivity against FLT3.
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| Cell Assay |
In vitro cellular assays are conducted to evaluate the functional activity of FLT3-IN-10. AML cell lines harboring FLT3 mutations are treated with the compound. Cell viability and proliferation are measured to assess the compound's anti-proliferative effects. FLT3 phosphorylation is also measured to confirm inhibition of the target kinase.
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| Animal Protocol |
In vivo animal experiments typically involve xenograft models of FLT3-mutated AML. Mice bearing these tumors are administered FLT3-IN-10. Tumor growth is monitored over time to assess the compound's efficacy. These studies are essential for demonstrating the in vivo antitumor activity of the compound.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of FLT3-IN-10 are typical of a small molecule inhibitor. Its molecular weight is 254.26. While detailed PK parameters are not widely published, its properties suggest it is designed to have favorable drug-like characteristics, including good permeability and metabolic stability, to support efficacy in vivo.
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| Toxicity/Toxicokinetics |
The toxicity profile of FLT3-IN-10 is not extensively documented but is likely to be similar to other FLT3 inhibitors. Common adverse effects may include myelosuppression, fatigue, and gastrointestinal disturbances. Preclinical studies would typically involve acute and chronic dosing in animal models to assess safety margins and identify potential target organ toxicities.
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| References | |
| Additional Infomation |
FLT3-IN-10 is a potent FLT3 inhibitor being studied for the treatment of FLT3-mutated acute myeloid leukemia (AML). It is a selective small-molecule inhibitor designed to block FLT3 signaling. The compound is a valuable research tool for studying the role of FLT3 in AML and for developing new therapeutic strategies.
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| Molecular Formula |
C15H11FN2O
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|---|---|
| Molecular Weight |
254.259046792984
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| Exact Mass |
254.085
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| CAS # |
2088735-51-5
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| PubChem CID |
162640986
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| Appearance |
Light yellow to light brown solid powder
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| LogP |
4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
19
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| Complexity |
275
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1C(C2=CC=C(F)C=C2)=CN=C1NC1=CC=CC=C1
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| InChi Key |
JNXCCEMGDXSTBQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H11FN2O/c16-12-8-6-11(7-9-12)14-10-17-15(19-14)18-13-4-2-1-3-5-13/h1-10H,(H,17,18)
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| Chemical Name |
5-(4-fluorophenyl)-N-phenyl-1,3-oxazol-2-amine
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: 125 mg/mL (491.62 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9330 mL | 19.6649 mL | 39.3298 mL | |
| 5 mM | 0.7866 mL | 3.9330 mL | 7.8660 mL | |
| 10 mM | 0.3933 mL | 1.9665 mL | 3.9330 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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