Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
IC50: 0.003 µM (FLT3)[1]
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ln Vitro |
FLT3-IN-18(compound 7d) decreases p-FLT3 Y589/591, p-FLT3 Y842, and p-in MV4-11 cells in a dose-dependent manner. This is demonstrated by the reduction of TAT5 Y694, p-ERK1/2 T202/Y204, p-MEK1/2 S217/221, and p-AKT S473 in protein expression [1]. Apoptosis and cell cycle arrest are induced in the G1 phase by FLT3-IN-18 (0, 0.01, 0.1, 1, 10, 100 nM; 24 h) [1].
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ln Vivo |
FLT3-IN-18 (10 mg/kg; ip; once) effectively inhibits FLT3 and STAT5 phosphorylation in rats[1].
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Cell Assay |
Cell Proliferation Assay[1]
Cell Types: MV4-11, K562, MOLM-13, Kasumi-1, THP-1, U937, MCF-7 cells Tested Concentrations: 0-20 µM Incubation Duration: 72 h Experimental Results: Inhibited cell growth with GI50s of 0.002, 0.380, 0.001, 0.513, 0.713, 0.664, 0.197 µM for MV4-11, K562, MOLM-13, Kasumi-1, THP-1, U937, MCF-7 cells, respectively. Western Blot Analysis[1] Cell Types: MV4-11 cells Tested Concentrations: 0, 0.01, 0.1, 1, 10, 100 nM Incubation Duration: 1 h Experimental Results: diminished the expression of p-FLT3 Y589/591, p-FLT3 Y842, p-TAT5 Y694, p -ERK1/2 T202/Y204, and p-MEK1/2 S217/221, p-AKT S473 in a dose-dependent manner. Cell Cycle Analysis[1] Cell Types: MV4-11 cells Tested Concentrations: 0, 0.01, 0.1, 1, 10, 100 nM Incubation Duration: 24 h Experimental Results: Induced cell cycle arrest at G1 phase. Apoptosis Analysis[1] Cell Types: MV4-11 cells Tested Concentrations: 0, 0.01, 0.1, 1, 10, 100 nM Incubation Duration: 24 h Experimental Results: Increased cleavage of the apoptotic marker protein PARP-1 (89 kDa fragment) and educed levels of the antiapoptotic protein Mcl-1. |
Animal Protocol |
Animal/Disease Models: Rats (MV4-11 xenografts)[1]
Doses: 10 mg/kg Route of Administration: Ip; once Experimental Results: Effectively inhibited FLT3-ITD autophosphorylation in MV4-11 xenografts, decreased STAT5 phosphorylation by over 95% after 24 h. |
References |
[1]. Gucký T, et al. Discovery of N2-(4-Amino-cyclohexyl)-9-cyclopentyl- N6-(4-morpholin-4-ylmethyl-phenyl)- 9H-purine-2,6-diamine as a Potent FLT3 Kinase Inhibitor for Acute Myeloid Leukemia with FLT3 Mutations. J Med Chem. 2018 May 10;61(9):3855-3869.
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Molecular Formula |
C26H36N8O
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Molecular Weight |
476.62
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CAS # |
752191-77-8
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SMILES |
N(C1C=CC(N2CCOCC2)=CC=1)C1N=C(N[C@@H]2CC[C@@H](N)CC2)N=C2N(C3CCCC3)C=NC=12
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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.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.0981 mL | 10.4905 mL | 20.9811 mL | |
5 mM | 0.4196 mL | 2.0981 mL | 4.1962 mL | |
10 mM | 0.2098 mL | 1.0491 mL | 2.0981 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.