| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
SKLB4771 (also known as FLT3-IN-1) is a novel, potent and selective inhibitor of FLT3 (fms-like tyrosine kinase 3) that may be potentially used for the treatment of cutaneous inflammation and psoriasis-like symptoms of disease. In a dose-dependent manner, SKLB4771 inhibited FLT3 phosphorylation. At concentrations >0.1 μM, there was a significant inhibition of the phosphorylation of STAT5 and ERK1/2, downstream signaling proteins, which is consistent with the downregulation of FLT3 phosphorylation. A single daily dosage of 100 mg/kg of SKLB4771 for eighteen days resulted in total tumor regression in an MV4-11 xenograft mouse model with no discernible side effects.
| Targets |
Flt3 (IC50 = 10 nM); Flt4 (IC50 = 3.7 μM); Aurora A (IC50 = 1.5 μM); c-kit (IC50 = 6.8 μM); FMS (IC50 = 2.8 μM)
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
In a dose-dependent manner, SKLB4771 inhibited the phosphorylation of FLT3. The phosphorylation of downstream signaling proteins STAT5 and ERK1/2 was also significantly inhibited at concentrations >0.1 μM, which is consistent with the downregulation of FLT3 phosphorylation.
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| Cell Assay |
In a 96-well plate, 1−4 × 104 leukemia cells are seeded per well, and each well is filled with an equal volume of medium containing escalating inhibitor concentrations. Following the 72-hour incubation period at 37°C, 20 μL of the 5 mg/mL MTT reagent is added to each well for a 2- to 4-hour incubation period, and the cells are lysed using 50 μL of 20% acidified SDS per well. Serial dilutions of inhibitors in culture medium are used to replace the medium after the other cell lines are seeded in 96-well plates at a density of 2.5 × 103 cells/well for 24 hours. After incubating for 72 hours, the cells are dissolved using 100% DMSO and then the MTT reagent is added and incubated for an additional 24 hours.
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| Animal Protocol |
female NOD-SCID mouse (6−7 weeks old)
20 mg/kg, 40 mg/kg, 100 mg/kg IV |
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| References |
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| Molecular Formula |
C25H27N7O3S2
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| Molecular Weight |
537.656981706619
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| Exact Mass |
537.162
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| Elemental Analysis |
C, 55.85; H, 5.06; N, 18.24; O, 8.93; S, 11.93
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| CAS # |
1370256-78-2
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| Related CAS # |
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| PubChem CID |
57412684
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.769
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
37
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| Complexity |
712
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| Defined Atom Stereocenter Count |
0
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| SMILES |
0
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| InChi Key |
LKXFSTAQMOENSC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H27N7O3S2/c1-17-3-5-18(6-4-17)28-23(33)29-24-30-31-25(37-24)36-22-20-8-7-19(15-21(20)26-16-27-22)35-12-2-9-32-10-13-34-14-11-32/h3-8,15-16H,2,9-14H2,1H3,(H2,28,29,30,33)
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| Chemical Name |
1-(4-methylphenyl)-3-[5-[7-(3-morpholin-4-ylpropoxy)quinazolin-4-yl]sulfanyl-1,3,4-thiadiazol-2-yl]urea
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.65 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 25.0 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: 2.5 mg/mL (4.65 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: ≥ 2.5 mg/mL (4.65 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 | 1.8599 mL | 9.2996 mL | 18.5991 mL | |
| 5 mM | 0.3720 mL | 1.8599 mL | 3.7198 mL | |
| 10 mM | 0.1860 mL | 0.9300 mL | 1.8599 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.
 J Med Chem.2012 Apr 26;55(8):3852-66. |
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