| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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Purity: ≥98%
| ln Vitro |
VLX600 (6 μM; 72 hours) promotes autophagy response [2]. VLX600 is cytotoxic to HCT116 spheroids. VLX600 induces HIF-1α-dependent glycolysis. VLX600 inhibits oxygen consumption in HCT116 cells. VLX600 suppresses the phosphorylation of mTOR downstream effectors 4EBP1 and p70-S6K through an HIF-1α-independent mechanism. VLX600 preferentially causes a decrease in ATP levels in cancer cells but not in normal cells [2].
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| ln Vivo |
In human tumor xenografts, VLX600 (16 mg/kg; intravenously; every three days for 16 days) demonstrated anticancer efficacy [2].
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| Cell Assay |
Cell proliferation experiment [2]
Cell Types: HCT116, HT29, SW620, HT8, DLD and RKO Cell Tested Concentrations: 0.1, 1, 10, 100μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibition of proliferation of these cells. Western Blot Analysis[2] Cell Types: HCT116 Cell Tested Concentrations: 6 μM Incubation Duration: 72 hrs (hours) Experimental Results: LC3-II was induced. |
| Animal Protocol |
Animal/Disease Models: NMRI nu/nu (nude) mice (HCT116 and HT29 colon cancer xenografts) [2]
Doses: 16 mg/kg Route of Administration: IV; every three days for 16 days Experimental Results: In HCT116 and HT29 colon Antitumor activity was observed in cancer xenografts. |
| References |
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| Additional Infomation |
OxPhos Inhibitor VLX600 is a lipophilic cation-based triazinoindolyl-hydrazone compound and mitochondrial oxidative phosphorylation (OxPhos) inhibitor, with potential antineoplastic activity. Upon infusion, in normal cells and proliferating tumor cells where glucose is readily available, inhibition of OxPhos by VLX600 induces a hypoxia-inducible factor 1-alpha (HIF-1alpha)-dependent shift to, and an increase in glycolysis. Glycolysis alone does not produce enough energy to support the growth of tumor cells in this environment, and the induction of autophagy occurs. In the metabolically compromised tumor microenvironment, the availability of oxygen and glucose is limited due to poor vascularization and perfusion of tumor micro-areas. Tumor cells growing in this environment are thus unable to compensate for decreased mitochondrial function by increasing glycolysis. This leads to nutrient depletion, decreased energy production, induction of autophagy, tumor cell death and an inhibition of cell proliferation in quiescent tumor cells. Mitochondrial OxPhos, which is hyperactivated in cancer cells, plays a key role in the promotion of cancer cell proliferation.
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| Molecular Formula |
C17H15N7
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|---|---|
| Molecular Weight |
317.348
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| Exact Mass |
317.138
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| CAS # |
327031-55-0
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| Related CAS # |
327031-55-0;1622945-04-3;VLX600 HCl;
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| PubChem CID |
6410104
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
24
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| Complexity |
468
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C2C(=CC=C1)C3=C(N2)N=C(N/N=C(\C)/C4=CC=CC=N4)N=N3
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| InChi Key |
UQOSBPRTQFFUOA-SRZZPIQSSA-N
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| InChi Code |
InChI=1S/C17H15N7/c1-10-6-5-7-12-14(10)19-16-15(12)22-24-17(20-16)23-21-11(2)13-8-3-4-9-18-13/h3-9H,1-2H3,(H2,19,20,23,24)/b21-11+
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| Chemical Name |
6-methyl-N-[(E)-1-pyridin-2-ylethylideneamino]-5H-[1,2,4]triazino[5,6-b]indol-3-amine
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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 Note: This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| 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) |
DMSO : ~25 mg/mL (~78.78 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (6.55 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1511 mL | 15.7555 mL | 31.5110 mL | |
| 5 mM | 0.6302 mL | 3.1511 mL | 6.3022 mL | |
| 10 mM | 0.3151 mL | 1.5755 mL | 3.1511 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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