Veledimex
Veledimex Basic information
- Product Name:
- Veledimex
- Synonyms:
-
- Veledimex (INXN-1001)
- RG-115932
- Benzoic acid, 2-ethyl-3-methoxy-, 2-(3,5-dimethylbenzoyl)-2-[(1R)-1-(1,1-dimethylethyl)butyl]hydrazide
- CAS:
- 1093130-72-3
- MF:
- C27H38N2O3
- MW:
- 438.6
- Mol File:
- 1093130-72-3.mol
Veledimex Chemical Properties
- Density
- 1.048±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 25 mg/mL (57.00 mM);Water : < 0.1 mg/mL (insoluble)
- form
- Solid
- pka
- 10.28±0.46(Predicted)
- color
- Light yellow to yellow
Veledimex Usage And Synthesis
Uses
Veledimex (INXN-1001), a synthetic analog of the insect molting hormone ecdysone, is an orally active activator ligand for a proprietary gene therapy promoter system. Veledimex can be used to activate certain genes using the ecdysone receptor (EcR)-based inducible gene regulation system, the RheoSwitch Therapeutic System (RTS). Veledimex can cross blood-brain barrier (BBB) in both orthotopic GL-261 mice and cynomolgus monkeys[1][2].
in vivo
Veledimex (INXN-1001) generally has moderate to low oral bioavailability after a single oral administration in mice and monkeys (-56% in mice and up to 17.4% in cynomolgus monkeys) with mostly low plasma clearance (1399 and 1170 mL/h per kilogram in mice and monkeys, respectively), high volume of distribution (20271 and 9180 mL/h per kilogram in mice and monkeys, respectively), and long terminal half-lives (-10 hours in mice and -30 hours in monkeys) after intravenous administration[1]. Ad-RTS-mIL-12 + Veledimex have demonstrated a dose-related increase in tumor IL-12 mRNA and IL-12 protein expression. Discontinuation of Veledimex resulted in a return to baseline IL-12 mRNA and protein expression in numerous syngeneic mouse tumor models. Veledimex crosses the blood-brain-barrier in both naive and orthotopic GL-261 mice with increased brain tissue level of -6 fold observed in tumor bearing vs. normal mice. Ad-RTS-mIL-12 + veledimex demonstrate a dose-related increase in survival without significant adverse events[2].
IC 50
IL-12; IL-1
References
[1] Barrett JA, et al. Regulated intratumoral expression of IL-12 using a RheoSwitch Therapeutic System? (RTS?) gene switch as gene therapy for the treatment of glioma. Cancer Gene Ther. 2018;25(5-6):106-116. DOI:10.1038/s41417-018-0019-0
[2] Chiocca EA, et al. Regulatable interleukin-12 gene therapy in patients with recurrent high-grade glioma: Results of a phase 1 trial. Sci Transl Med. 2019;11(505):eaaw5680. DOI:10.1126/scitranslmed.aaw5680
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