Adilipoline™ (CL413)

Bispecific TLR2 & TLR7 ligand

Adilipoline™ (S-(2,3-bis(palmitoyloxy)- (2RS)propyl)- (R)-cysteinyl-(S)-seryl-(S)- lysyl- (S)-lysyl- (S)-lysyl- (S)-lysyl 4 -((6-amino-2- (butylamino)-8- hydroxy-9H- purin-9-yl) methyl) aniline) was generated by conjugation of an 8-hydroxyadenine moiety to the terminal acid function of Pam2CSK4, a TLR2 agonist.

Adilipoline™ is a good ligand for both TLR2 and TLR7. In vivo tumor studies have demonstrated that Adilipoline™ is a potent antitumor agent. Intratumoral injection of Adilipoline™ in established B16 tumors resulted in tumor regression.

Specifications

Specificity: TLR2 and TLR7 agonist

Synonym: S-(2,3-bis (palmitoyloxy)-(2RS) propyl)- (R)-cysteinyl- (S)-seryl- (S)-lysyl- (S)-lysyl- (S)-lysyl-(S)- lysyl 4-((6-amino-2- (butylamino)-8-hydroxy- 9H-purin-9-yl)methyl) aniline

Working concentration: 50 pg- 10 µg/ml (~30 pM - 10 µM)

Solubility: H₂O (1 mg/ml)

Formula: C₈₁H₁₄₅N₁₇O₁₂S

Molecular weight: 1581 g/mol

Quality Control: 

• Purity: ≥95% (UHPLC)
• TLR2 and TLR7 activity has been confirmed using cellular assays.
• The absence of bacterial contamination (e.g. endotoxins) has been confirmed using HEK‑Blue™ TLR4 cells.

Contents

• 500 µg Adilipoline™ (CL413)
• 1.5 ml endotoxin-free water

Products are shipped at room temperature.

 Upon receipt, store at -20°C.

Description

Details

HEK-Blue™ hTLR2 cells  which stably express an NF-κB-inducible SEAP reporter gene and human TLR2 were incubated in HEK-Blue™ Detection (a SEAP detection growth medium) and stimulated with increasing concentrations of the agonists indicated in the graph.
After 24h incubation, the levels of NF-κB-induced SEAP were determined by reading the OD at 655 nm.

HEK-Blue™ hTLR7 cells, which stably express an NF-κB-inducible SEAP reporter gene and human TLR7 were incubated in HEK-Blue™ Detection (a SEAP detection growth medium) and stimulated with increasing concentrations of the agonists indicated in the graph.
After 24h incubation, the levels of NF-κB-induced SEAP were determined by reading the OD at 655 nm.

RAW-Blue™ cells, which stably express an NF-κB-inducible SEAP reporter gene, were stimulated with 0.6 µg/ml of InvivoGen’s multi-PRR ligands complexed with 0.1 µg/ml HSV-60 (synthetic dsDNA).
After 24h incubation, the levels of NF-κB-induced SEAP were determined using QUANTI-Blue™, a SEAP detection reagent.

(A) Tumor growth after CL413 or CL401 treatment. C57BL/6 mice were inoculated subcutaneously with 5x10e5 B16-F1 mouse melanoma cells. After seven days, Adilipoline™ (CL413), CL401 or vehicle were injected intratumorally (50 µg/mouse/50 µl) on days 5, 15 and 20. (B) Survival curves for untreated as well as CL413- or CL401-treated mice.

Each group contained 8 mice. Black arrows represent the days of injection. Tumor growth was monitored and measured with calipers after day 5 of grafting tumor cells into mice and then every 2 days thereafter. Tumor volume in mm3 was determined according to the formula V = W2 x L/2, where L = length (mm) and W = width (mm).