| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
Class III receptor tyrosine kinases, including FLT3 (Fms-like tyrosine kinase 3), c-Kit, c-Fms (colony-stimulating factor 1 receptor), and PDGFRβ (platelet-derived growth factor receptor beta). It is an ATP-competitive inhibitor.
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| ln Vitro |
GTP-14564 inhibits the growth of interleukin-3-independent Ba/F3 cells expressing ITD-FLT3 (internal tandem duplication mutant) at 1 µM. A 30-fold higher concentration (30 µM) is required to inhibit FLT3 ligand-dependent growth of Ba/F3 cells expressing wild-type FLT3 (wt-FLT3). This demonstrates selectivity for the mutant FLT3 over the wild-type receptor.
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| ln Vivo |
Specific in vivo activity data for GTP-14564 are not detailed in the available literature. As a kinase inhibitor, its in vivo efficacy could be evaluated in xenograft models of FLT3-dependent leukemia. However, specific studies are not described.
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| Enzyme Assay |
The in vitro kinase inhibition assay for GTP-14564 typically involves measuring the activity of recombinant class III RTKs (FLT3, c-Kit, c-Fms, PDGFRβ) in the presence of varying concentrations of the compound. The enzyme is incubated with ATP and a substrate peptide, and the phosphorylation of the substrate is quantified. The IC50 value is determined from the dose-response curve. Selectivity is assessed by testing the compound against a panel of related kinases.
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| Cell Assay |
Specific in vitro cell-based assay protocols for GTP-14564 are described for Ba/F3 cells expressing ITD-FLT3 or wt-FLT3. Cells are cultured in the presence of IL-3 or FLT3 ligand, respectively. GTP-14564 is added at various concentrations, and cell growth is measured after a defined period (e.g., 72 hours) using a cell viability assay such as MTT or CellTiter-Glo. The concentration inhibiting 50% of cell growth (IC50) is determined.
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| Animal Protocol |
Specific in vivo animal model protocols for GTP-14564 are not described. To evaluate its in vivo efficacy, GTP-14564 could be administered to mouse xenograft models of FLT3-mutant leukemia. Tumor-bearing mice would be treated with GTP-14564 (e.g., orally or intraperitoneally), and tumor growth inhibition would be monitored. Endpoints would include tumor volume measurement and survival analysis.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for GTP-14564 are not reported in the available literature. As a research compound, its absorption, distribution, metabolism, and excretion (ADME) properties have not been extensively characterized. Studies would be needed to determine its bioavailability, half-life, and protein binding.
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| Toxicity/Toxicokinetics |
Specific toxicological data for GTP-14564 are not available. As a research compound, its safety profile has not been comprehensively characterized. Toxicity studies would be required to determine its safety margin and potential off-target effects.
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| References | |
| Additional Infomation |
3-Phenylacetyl-1H-benzofurano[3,2-c]pyrazole is a pyrazole compound and a cyclic compound.
GTP-14564 is a research tool for studying class III RTK signaling, particularly FLT3 and its role in leukemia. Its selectivity for ITD-FLT3 over wt-FLT3 makes it a valuable compound for investigating the mechanisms of FLT3 inhibitor resistance and for developing more selective therapeutic agents. It is not an approved therapeutic agent. |
| Molecular Formula |
C15H10N2O
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|---|---|
| Molecular Weight |
234.25
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| Exact Mass |
234.079
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| CAS # |
34823-86-4
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| PubChem CID |
3385203
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.321g/cm3
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| Boiling Point |
459.1ºC at 760mmHg
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| Flash Point |
240.7ºC
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| Index of Refraction |
1.738
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| LogP |
3.976
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
18
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| Complexity |
303
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DZQLVVLATXPWBK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H10N2O/c1-2-6-10(7-3-1)13-15-14(17-16-13)11-8-4-5-9-12(11)18-15/h1-9H,(H,16,17)
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| Chemical Name |
3-phenyl-1H-[1]benzofuro[3,2-c]pyrazole
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| Synonyms |
GTP-14564; GTP 14564; GTP14564
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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 : ~125 mg/mL (~533.62 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 | 4.2689 mL | 21.3447 mL | 42.6894 mL | |
| 5 mM | 0.8538 mL | 4.2689 mL | 8.5379 mL | |
| 10 mM | 0.4269 mL | 2.1345 mL | 4.2689 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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