Size | Price | Stock | Qty |
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1mg |
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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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Targets |
Pan-FLT3/Pan-BTK[1]
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ln Vitro |
Luxeptinib suppresses cell growth with an IC50 of 32 nM (MEC-1 CLL cells; 0.1~10 μM; 72 hours)[1]. In primary chronic lymphocytic leukemia (CLL) cells, luxeptinib phosphorylates S6 ribosomal protein, ERK1/2, BTK, PLCg2, AKT, and SYK, and it also substantially inhibits SYK phosphorylation [1]. The phosphorylation of FLT3 and STAT5 is entirely inhibited by luxeptinib (MV4-11 cells; 500 pM; 1 hour) [2].
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Cell Assay |
Cell Proliferation Assay[1]
Cell Types: MEC-1 CLL cells Tested Concentrations: 0.1~10 µM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited cells proliferation with an IC50 of 32 nM. |
References |
[1]. Ekaterina Kim MS, et al. CG-806, a First-in-Class Pan-FLT3/Pan-BTK Inhibitor, Exhibits Broad Signaling Inhibition in Chronic Lymphocytic Leukemia Cells. bloodjournal Blood blood (2019). 134 (Supplement_1) : 3051.
[2]. Abstract 44: CG′806, a first-in-class FLT3/BTK inhibitor, exhibits potent activity against AML patient samples with mutant or wild type FLT3, as well as other hematologic malignancy subtypes [3]. Guopan Yu,et al.CG '806, a Novel Pan-FLT3/BTK Multi-Kinase Inhibitor, Induces Cell Cycle Arrest, Apoptosis or Autophagy in AML Cells Depending on FLT3 Mutation Status. Blood blood (2017).130 (Suppl_1) : 462 [4]. Aptose Biosciences to Present CG’806 Data at AACR Hematologic Malignancies Meeting |
Molecular Formula |
C25H17F4N5O2
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Molecular Weight |
495.43
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CAS # |
1616428-23-9
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
FC1C=C(C=CC=1C1=CC=C(C2=NC=C(C)N2)C2C(NCC=21)=O)NC(NC1C(=CC(=CC=1F)F)F)=O
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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 : 50 mg/mL (100.92 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.05 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 sonication.
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. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.20 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.20 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 | 2.0184 mL | 10.0922 mL | 20.1845 mL | |
5 mM | 0.4037 mL | 2.0184 mL | 4.0369 mL | |
10 mM | 0.2018 mL | 1.0092 mL | 2.0184 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.