[CAS NO. 870087-36-8] Apilimodmesylate
PRODUCTS SPECIFICATIONS [870087-36-8]
DESCRIPTION [870087-36-8]
Overview
| MDL | MFCD28167749 |
|---|---|
| Molecular Weight | 610.70 |
| Molecular Formula | C25H34N6O8S2 |
| SMILES | CC1=CC=CC(/C=N/NC2=CC(N3CCOCC3)=NC(OCCC4=CC=CC=N4)=N2)=C1.CS(=O)(O)=O.CS(=O)(O)=O |
12 Publications Citing Use of MCE
- [1]Sci Adv. 2022 Jul 22;8(29):eabn1440.
- [2]Nat Commun. 2020 Mar 27;11(1):1620.
- [3]Biomaterials. 2022 Jun;285:121509.
- [4]Theranostics. 2020 Mar 4;10(9):3925-3938.
- [5]Cell Mol Life Sci. 2016 Dec;73(24):4717-4737.
- [6]Br J Cancer. 2020 Aug;123(4):542-555.
- [7]J Virol. 2021 Aug 18;JVI0097521.
- [8]J Biol Chem. 2022 Dec 6;102775.
- [9]Commun Biol. 2022 Mar 24;5(1):262.
- [10]Biotechnol J. 2022 Dec 7;e2200147.
- [11]Viruses. 2021 Jun 28;13(7):1255.
- [12]bioRxiv. 2020 Apr 21;2020.04.21.053058.
Summary
IC50 & Target
|
IL-12 |
IL-23 |
In Vitro
Apilimod inhibits IFN-γ production induced by either IFN-γ/SAC or SAC in human PBMCs, with an IC 50 of approximately 20 nM. Apilimod show some inhibition against IFN-γ/SAC-induced TNF-α and ConA-induced IL-5 from human PBMCs at high concentrations, but no suppressive effect against IL-1β, IL-2, IL-4, IL-8, and IL-18 in all cultures tested. The p35 and p40 promoter-driven luciferase activities are significantly induced after stimulation with IFN-γ/LPS or IFN-γ/SAC, and are completely suppressed by 100 nM Apilimod [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Apilimod (10 mg/kg, p.o.) is effective not only when administered throughout the entire experiment, but also when administration is initiated on day 30 when disease is clearly measurable but not maximal. Apilimod causes a significant reduction in cell number only in the Th1 model, with an average percentage of inhibition of 51%±8% relative to the vehicle control. Apilimod treatment has no effect in the Th2 setting [1] . Apilimod (5 or 20 mg/kg, p.o.) reduces the level of IL-12 p40 in serum without altering body weight in EAU mice. Oral administration of Apilimod reduces the severity of experimental autoimmune uveoretinitis (EAU) by clinical and histopathological analysis [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04446377 | AI Therapeutics, Inc.|Yale University |
COVID-19 Disease
|
July 15, 2020 | Phase 2 |
| NCT00642629 | Synta Pharmaceuticals Corp. |
Active, Moderate to Severe Rheumatoid Arthritis
|
December 2005 | Phase 2 |
| NCT00250198 | National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) |
Crohn´s Disease
|
November 3, 2005 | Phase 2 |
| NCT00263237 | National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) |
Common Variable Immunodeficiency
|
December 2, 2005 | Phase 1 |
| NCT00234741 | Synta Pharmaceuticals Corp.|National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health (NIH) |
Crohn´s Disease
|
November 2005 | Phase 2 |
| NCT00138840 | Synta Pharmaceuticals Corp. |
Crohn´s Disease
|
August 2005 | Phase 2 |
| NCT00088062 | Synta Pharmaceuticals Corp. |
Crohn´s Disease
|
February 2004 | Phase 1|Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 100 mg/mL ( 163.75 mM ; Need ultrasonic)
DMSO : 12.5 mg/mL ( 20.47 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
-
1.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (163.75 mM); Clear solution; Need ultrasonic
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.25 mg/mL (2.05 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 1.25 mg/mL (2.05 mM); Clear solution
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] Billich A. Drug evaluation: apilimod, an oral IL-12/IL-23 inhibitor for the treatment of autoimmune diseases and common variable immunodeficiency.IDrugs. 2007 Jan;10(1):53-9.
- [3] 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.