| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Interleukin-12 (IL-12) is a pro-inflammatory cytokine that is crucial for generating anti-cancer immune responses. Ad-RTS-IL-12 is an adenoviral vector designed to express hIL-12. Veledimex is an orally active small molecule dihydrazide that modulates the expression of target genes. The amount of gene product generated systemically and the duration of activity depend on the dose level and length of administration of veledimex [1].
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|---|---|
| ln Vivo |
Phase I/II clinical trials are being conducted on Veledimex in combination with Ad-RTS-hIL-12 to treat breast cancer and melanoma. Ad-RTS-mIL-12 administered intratumorally and veledimex administered orally produced dose-dependent anticancer effects in mouse melanoma, breast cancer, and glioma models. These effects were linked to increased veledimex plasma exposure. Ad-RTS-mIL-12 combined with increases in tumor veledimex levels caused a dose-dependent rise (switching on) of IL-12 mRNA, which in turn caused a dose-dependent increase in IL-12p70 in tumors, whereas IL-12p70 raised minimum blood IL-12. Ad-RTS-mIL-12 + veledimex-induced dose-related reduction in breast cancer and melanoma is the result of increased tumor IL-12, which is linked to an increase in tumor CD8+ cytotoxic T cells and a decrease in regulatory T cells in the tumor microenvironment. Growth rate and body weight in tumor syngeneic mouse models were not significantly altered. Veledimex has a moderate to low oral bioavailability (up to 17.4% in cynomolgus monkeys and 56% in mice) following a single oral dose. It also has a very low plasma clearance (1399 and 1170 mL/h/kg in mice and monkeys, respectively), a high volume of distribution following intravenous administration (20271 and 9180 mL/h/kg in mice and monkeys, respectively), and a long terminal half-life (-10 hours in mice and 30 hours in monkeys)[1].
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| References |
| Molecular Formula |
C27H38N2O3
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|---|---|
| Molecular Weight |
438.602227687836
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| Exact Mass |
438.288
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| CAS # |
755013-59-3
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| Related CAS # |
Veledimex;1093130-72-3;Veledimex (S enantiomer);1093131-03-3
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| PubChem CID |
66558029
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| Appearance |
White to off-white solid powder
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| Density |
1.0±0.1 g/cm3
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| Index of Refraction |
1.541
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| LogP |
6.2
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| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
8
|
| Heavy Atom Count |
32
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| Complexity |
605
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| Defined Atom Stereocenter Count |
0
|
| InChi Key |
LZWZPGLVHLSWQX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H38N2O3/c1-9-12-24(27(5,6)7)29(26(31)20-16-18(3)15-19(4)17-20)28-25(30)22-13-11-14-23(32-8)21(22)10-2/h11,13-17,24H,9-10,12H2,1-8H3,(H,28,30)
|
| Chemical Name |
N'-(3,5-dimethylbenzoyl)-N'-(2,2-dimethylhexan-3-yl)-2-ethyl-3-methoxybenzohydrazide
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| Synonyms |
INXN-1001 racemate; RG-115932 racemate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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