[CAS NO. 1093130-72-3]  Veledimex

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PRODUCTS SPECIFICATIONS [1093130-72-3]

Fulfillment
Catalog
AS904643
Brand
Arctom Scientific
CAS
1093130-72-3

DESCRIPTION [1093130-72-3]

Overview

MDL-
Molecular Weight438.60
Molecular FormulaC27H38N2O3
SMILESO=C(NN(C(C1=CC(C)=CC(C)=C1)=O)[C@@H](C(C)(C)C)CCC)C2=CC=CC(OC)=C2CC

For research use only. We do not sell to patients.

Summary

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] .


IC50 & Target

IL-12


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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT02423902 Alaunos Therapeutics
Metastatic Breast Cancer
July 2015 Phase 1|Phase 2
NCT04006119 Alaunos Therapeutics
Glioblastoma
August 1, 2019 Phase 2
NCT01397708 Alaunos Therapeutics
Melanoma
August 2011 Phase 1|Phase 2

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL ( 57.00 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2800 mL 11.3999 mL 22.7998 mL
5 mM 0.4560 mL 2.2800 mL 4.5600 mL
10 mM 0.2280 mL 1.1400 mL 2.2800 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.70 mM); Clear solution

* All of the co-solvents are available by MCE.