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Purity: ≥98%
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. In the Th1 model alone, TA-5326 significantly decreased the number of cells, with an average percent inhibition of 51% ± 8% in comparison 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 |
[1]. Wada Y, et al. Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL-23 inhibitor. Blood. 2007 Feb 1;109(3):1156-64.
[2]. Keino H, et al. Therapeutic effect of the potent IL-12/IL-23 inhibitor STA-5326 on experimental autoimmune uveoretinitis. Arthritis Res Ther. 2008;10(5):R122 |
| Molecular Formula |
C23H26N6O2
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|---|---|
| Molecular Weight |
418.4915
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| CAS # |
541550-19-0
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| Related CAS # |
Apilimod mesylate;870087-36-8
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| SMILES |
O1C([H])([H])C([H])([H])N(C2C([H])=C(N([H])N=C([H])C3=C([H])C([H])=C([H])C(C([H])([H])[H])=C3[H])N=C(N=2)OC([H])([H])C([H])([H])C2=C([H])C([H])=C([H])C([H])=N2)C([H])([H])C1([H])[H]
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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 : ~100 mg/mL (~238.95 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.97 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 (5.97 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 3.33 mg/mL (7.96 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3895 mL | 11.9477 mL | 23.8954 mL | |
| 5 mM | 0.4779 mL | 2.3895 mL | 4.7791 mL | |
| 10 mM | 0.2390 mL | 1.1948 mL | 2.3895 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.
Apilimod selectively inhibits TLR-induced cytokine expression.Chem Biol.2013 Jul 25;20(7):912-21. |
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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