Apilimod dimesylate

Apilimod dimesylate, also known as STA-5326, is a IL-12/IL-23 inhibitor. Apilimod inhibits IL-12 and IL-23 production - cytokines that are involved in autoimmune diseases - through the prevention of nuclear translocation of c-Rel. Synta Pharmaceuticals Corp is developing apilimod for the potential treatment of Crohn's disease (CD) and other autoimmune diseases. Preclinical studies demonstrated the successful inhibition of IL-12 and IL-23 production by the drug.

Product information

CAS Number: 870087-36-8

Molecular Weight: 610.70

Formula: C25H34N6O8S2

Synonym:

STA-5326

LAM-002

Apilimod

Chemical Name:  (E)-4-(6-(2-(3-methylbenzylidene)hydrazinyl)-2-(2-(pyridin-2-yl)ethoxy)pyrimidin-4-yl)morpholine dimethanesulfonate

Smiles: CC1C=CC=C(C=1)/C=N/NC1=CC(=NC(=N1)OCCC1=CC=CC=N1)N1CCOCC1.CS(O)(=O)=O.CS(O)(=O)=O

InChiKey: GAJWNIKZLYZYSY-OKUPSQOASA-N

InChi: 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+;;

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

References:

1. Cai X, Xu Y, Kim YM, Loureiro J, Huang Q. PIKfyve, a class III lipid kinase, is required for TLR-induced type I IFN production via modulation of ATF3. J Immunol. 2014 Apr 1;192(7):3383-9. doi: 10.4049/jimmunol.1302411. Epub 2014 Mar 5. PubMed PMID: 24600036.
2. Baird AM, Dockry E, Daly A, Stack E, Doherty DG, O'Byrne KJ, Gray SG. IL-23R is Epigenetically Regulated and Modulated by Chemotherapy in Non-Small Cell Lung Cancer. Front Oncol. 2013 Jun 19;3:162. doi: 10.3389/fonc.2013.00162. eCollection 2013. PubMed PMID: 23802098; PubMed Central PMCID: PMC3685824.
3. Wada Y, Cardinale I, Khatcherian A, Chu J, Kantor AB, Gottlieb AB, Tatsuta N, Jacobson E, Barsoum J, Krueger JG. Apilimod inhibits the production of IL-12 and IL-23 and reduces dendritic cell infiltration in psoriasis. PLoS One. 2012;7(4):e35069. doi: 10.1371/journal.pone.0035069. Epub 2012 Apr 6. PubMed PMID: 22493730; PubMed Central PMCID: PMC3320873.

Products are for research use only. Not for human use.