| 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 |
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| ln Vitro |
SKLB4771 (compound 20c) has a 72-hour half-life of 6 nM, which is sufficient to suppress FLT3-ITD-expressing MV4-11 cells. Additionally, various cancer cells had IC50 values of 3.05 μM, 6.25 μM, 3.72 μM, 6.94 μM (H292), and 8.91 μM (A431), respectively [1]. At doses >0.1 μM, SKLB4771 (0-300 nM; 20 hours) decreases the phosphorylation of downstream signaling proteins STAT5 and ERK1/2 and suppresses FLT3 phosphorylation [1].
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| ln Vivo |
In vivo tumor growth was suppressed by SKLB4771 (20–100 mg/kg; i.p.; once daily; 21 days) in mice without causing appreciable weight loss or other clear indicators of toxicity [1]. Rats' 40 mg/kg intraperitoneal (ip) pharmacokinetic study of SKLB4771[1] Cmax (μg/mL) T1/2 (h) AUCmax (h·μg/mL) Tmax (h) CLobs (L/h/kg) 5.31 13.9 21.86 1.0 2.21
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: MV4-11 Cell Tested Concentrations: 0, 30, 100, 300 nM Incubation Duration: 20 hrs (hours) Experimental Results: Inhibits human FLT3 kinase in a dose-dependent manner and reduces the phosphorylation level of FLT3 kinase 100 nM and 300 nM of STAT5 and ERK1/2. |
| Animal Protocol |
Animal/Disease Models: Female NOD-SCID (severe combined immunodeficient) mouse (6−7 weeks old) [1]
Doses: 20, 40, 100 mg/kg; dissolved in 25% (v/v) PEG400 plus Administer at a dose of 5 mL/kg in 5% DMSO. one time/day; 21-day Experimental Results: 20 mg/kg and 40 mg/kg inhibited tumor growth by 66% and 84% respectively. Resulting in inhibition of cell proliferation and induction of apoptosis. |
| References |
[1]. Li WW, et al. Discovery of the novel potent and selective FLT3 inhibitor 1-{5-[7-(3- morpholinopropoxy)quinazolin-4-ylthio]-[1,3,4]thiadiazol-2-yl}-3-p-tolylurea and its anti-acute myeloid leukemia (AML) activities in vitro and in vivo. J Med Chem. 2012 Apr 26;55(8):3852-66.
[2]. Yan HX, et al. Accumulation of FLT3(+) CD11c (+) dendritic cells in psoriatic lesions and the anti-psoriatic effect of a selective FLT3 inhibitor. Immunol Res. 2014 Oct;60(1):112-26. |
| Molecular Formula |
C25H27N7O3S2
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|---|---|
| Molecular Weight |
537.66
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| Exact Mass |
537.1617
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| CAS # |
1370256-78-2
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
CC1=CC=C(C=C1)NC(=O)NC2=NN=C(S2)SC3=NC=NC4=C3C=CC(=C4)OCCCN5CCOCC5
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| Synonyms |
SKLB 4771. FLT3-IN-1; SKLB-4771; SKLB4771
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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 : ~33.33 mg/mL (~61.99 mM)
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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.
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