| Size | Price | Stock | Qty |
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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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| 500mg |
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| 1g |
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| Other Sizes |
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Purity: ≥98%
Apilimod mesylate, the mesylate salt of Apilimod, is a novel and potent small molecular inhibitor of IL-12/IL-23 and has been evaluated in clinical trials for patients with Crohn's disease or rheumatoid arthritis. Using a chemical genetic approach, Apilimod was shown to bind to PIKfyve and block its phosphotransferase activity, leading to selective inhibition of IL-12/IL-23p40. Pharmacological or genetic inactivation of PIKfyve is necessary and sufficient for suppression of IL-12/IL-23p40 expression. Apilimod, a candidate of anticancer therapeutic, arrests not only PtdIns(3,5)P2 but also PtdIns5P synthesis by PIKfyve and induces bafilomycin A1-reversible aberrant endomembrane dilation.
| ln Vitro |
Apilimod has an IC50 of about 20 nM, which suppresses IFN-γ/SAC or SAC-induced IFN-γ production in human PBMC. On TNF-α generated by IFN-γ/SAC and IL-5 caused by ConA in high-concentration human PBMC, Apimod exhibits a certain amount of inhibitory action; nevertheless, in all cultures examined, it exhibits a certain amount of inhibitory action on IL-1β, IL-2, IL-4, IL-8, and IL-18. IFN-γ/LPS or IFN-γ/SAC stimulation greatly increased luciferase activity fueled by the p35 and p40 promoters, whereas 100 nM Apilimod totally blocked it [1].
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| ln Vivo |
Not only did apimod (10 mg/kg, po) work well when given continuously during the trial, but it also worked well when started on day 30, when the disease was manifestly detectable but not at its worst. Only in the Th1 model did Apimod significantly reduce the number of cells; on average, 51% ± 8% less cells were inhibited compared to the vehicle control. Patients with Th2 do not respond to apimod therapy [1]. In EAU mice, apilimimod (5 or 20 mg/kg) decreases blood IL-12 p40 levels without affecting body weight. Clinical and histological investigation shows that oral apimod lowers the severity of experimental autoimmune uveoretinitis (EAU) [2].
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| References |
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| Molecular Formula |
C25H34N6O8S2
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|---|---|
| Molecular Weight |
610.7029
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| Exact Mass |
610.187
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| CAS # |
870087-36-8
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| Related CAS # |
Apilimod;541550-19-0
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| PubChem CID |
11527330
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
41
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| Complexity |
637
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC(=CC=C1)/C=N/NC2=CC(=NC(=N2)OCCC3=CC=CC=N3)N4CCOCC4.CS(=O)(=O)O.CS(=O)(=O)O
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| InChi Key |
GAJWNIKZLYZYSY-OKUPSQOASA-N
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| InChi Code |
InChI=1S/C23H26N6O2.2CH4O3S/c1-18-5-4-6-19(15-18)17-25-28-21-16-22(29-10-13-30-14-11-29)27-23(26-21)31-12-8-20-7-2-3-9-24-20;2*1-5(2,3)4/h2-7,9,15-17H,8,10-14H2,1H3,(H,26,27,28);2*1H3,(H,2,3,4)/b25-17+;;
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| Chemical Name |
(E)-4-(6-(2-(3-methylbenzylidene)hydrazinyl)-2-(2-(pyridin-2-yl)ethoxy)pyrimidin-4-yl)morpholine dimethanesulfonate
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| Synonyms |
LAM-002; LAM 002; STA-5326; STA5326; STA 5326; LAM002; Apilimod mesylate.
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O : ~100 mg/mL (~163.75 mM)
DMSO : ~12.5 mg/mL (~20.47 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.05 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 12.5 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: ≥ 1.25 mg/mL (2.05 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 12.5 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: ≥ 1.25 mg/mL (2.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (163.75 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6375 mL | 8.1873 mL | 16.3747 mL | |
| 5 mM | 0.3275 mL | 1.6375 mL | 3.2749 mL | |
| 10 mM | 0.1637 mL | 0.8187 mL | 1.6375 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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Apilimod binds to and inhibits PIKfyve kinase activity.Chem Biol.2013 Jul 25;20(7):912-21. |
Apilimod inhibits PIKfyve kinase activity in cells.Chem Biol.2013 Jul 25;20(7):912-21. |
PIKfyve modulates TLR-induced IL12p40 expression.Chem Biol.2013 Jul 25;20(7):912-21. |
BafA1 suppresses PtdIns3P elevation but does not mitigate PtdIns(3,5)P2reduced by apilimod.PLoS One. 2018; 13(9): e0204532. |
BafA1 precludes EEA1 membrane recruitment induced by PIKfyve inhibition with apilimod.PLoS One. 2018; 13(9): e0204532. |
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