Veledimex racemate (RG-115932 racemate) (Synonyms: INXN-1001 racemate; RG-115932 racemate) |
Catalog No.GC33870
One-Click Copy Product Info
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Veledimex racemate (RG-115932 racemate) (INXN-1001 racemate) is the racemate of veledimex.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 755013-59-3
Sample solution is provided at 25 µL, 10mM.
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Veledimex racemate is the racemate of veledimex. Veledimex is an orally available, small-molecule activator ligand for the RheoSwitch Therapeutic System.
Interleukin 12 (IL-12) is a pro-inflammatory cytokine critical for stimulating anti-cancer immune responses. Ad-RTS-IL-12 is the adenovirusvector engineered to express hIL-12. Veledimex is an orally active small-molecule diacylhydrazine and controls the expression of the target gene. The amount of gene product produced by the system and the duration of the effect are dependent on veledimex dose level and duration of dosing[1].
Veledimex, combined with Ad-RTS-hIL-12, is in phase I/II clinical trials for the treatment of melanoma and breast cancer. Intratumoral administration of Ad-RTS-mIL-12 along with oral administration of veledimex elicits dose-dependent antitumor effects in murine melanoma, breast cancer, and glioma models, which correlates with increased plasma exposure of veledimex. The increase in tumor veledimex levels in combination with Ad-RTS-mIL-12 results in a dose-related increase in the IL-12 mRNA (switch on) leading to dose-related increases in IL-12p70 in the tumor with minimal increase in serum IL-12. The increase in tumor IL-12 correlates with an increase in tumor CD8+ cytotoxic T cells and a concomitant decrease in regulatory T cells in the tumor microenvironment, which leads to Ad-RTS-mIL-12 + veledimex-elicited dose-related decreases in tumor growth rate with no significant change in body weight in both breast and melanoma syngeneic mouse models. Veledimex 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].
[1]. Cai H, et al. Plasma Pharmacokinetics of Veledimex, a Small-Molecule Activator Ligand for a Proprietary GeneTherapy Promoter System, in Healthy Subjects. Clin Pharmacol Drug Dev. 2017 May;6(3):246-257.
| Cas No. | 755013-59-3 | SDF | |
| Synonyms | INXN-1001 racemate; RG-115932 racemate | ||
| Canonical SMILES | O=C(NN(C(C1=CC(C)=CC(C)=C1)=O)C(C(C)(C)C)CCC)C2=CC=CC(OC)=C2CC | ||
| Formula | C27H38N2O3 | M.Wt | 438.6 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.28 mL | 11.3999 mL | 22.7998 mL |
| 5 mM | 456 μL | 2.28 mL | 4.56 mL |
| 10 mM | 228 μL | 1.14 mL | 2.28 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)