| Size | Price | Stock | Qty |
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| 1mg |
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| Targets |
OXi8007 targets tubulin, acting as a prodrug that is converted to the active tubulin-binding compound OXi8006. As a vascular disrupting agent, it disrupts microtubules in tumor endothelial cells, leading to tumor vascular collapse and reduced blood flow to tumors. This mechanism results in tumor cell death and inhibition of tumor growth.
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| ln Vitro |
In vitro, OXi8007 acts as a vascular disrupting agent with potent anticancer activity. It exhibits strong cytotoxicity against selected human cancer cell lines, with a GI50 of 36 nM against DU-145 cells. As a prodrug of OXi8006, it is converted to the active tubulin-binding compound in cells.
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| ln Vivo |
In vivo activity of OXi8007 has been demonstrated in preclinical models, where it significantly disrupts the tumor vascular system. As a vascular disrupting agent, it reduces tumor blood flow and inhibits tumor growth. Its water-soluble phosphate prodrug design enhances its bioavailability and delivery to tumor tissues.
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| Enzyme Assay |
The in vitro tubulin binding assay for OXi8007 involves measuring its interaction with tubulin following conversion to its active form, OXi8006. These assays use purified tubulin protein and measure the extent of tubulin polymerization in the presence of the active compound. The prodrug OXi8007 is converted to OXi8006, which binds to tubulin and inhibits microtubule assembly.
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| Cell Assay |
In vitro cellular assays for OXi8007 are performed using cancer cell lines such as DU-145 prostate cancer cells. These assays measure the compound's cytotoxicity using standard cell viability assays, with a GI50 of 36 nM against DU-145 cells. The compound's effects on microtubule organization are assessed by immunofluorescence staining of tubulin. These assays demonstrate its potent anticancer activity.
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| Animal Protocol |
In vivo animal studies for OXi8007 are conducted in mouse xenograft models of various cancers. These studies typically involve administration of the compound, followed by assessment of tumor growth inhibition and tumor vascular disruption. The compound's ability to significantly disrupt the tumor vascular system and inhibit tumor growth is evaluated. Its water-soluble prodrug design enhances its bioavailability.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of OXi8007 are characterized by its water-soluble phosphate prodrug design, which enhances its bioavailability and delivery to tumor tissues. As a prodrug of OXi8006, it is converted to the active compound in vivo, which exerts the vascular-disrupting effects. Its pharmacokinetic profile supports its use as an anticancer agent.
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| Toxicity/Toxicokinetics |
Toxicology studies of OXi8007 have been conducted to evaluate its safety profile as a vascular disrupting agent. These studies include acute and repeat-dose toxicity assessments in preclinical species, as well as evaluations of cardiovascular function. As a tubulin-binding compound, its toxicology profile includes effects on rapidly dividing cells and vascular function.
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| References | |
| Additional Infomation |
OXi8007 is a water-soluble phosphate prodrug of OXi8006, a tubulin-binding compound, with potential anticancer activity. As a vascular disrupting agent, it exhibits strong cytotoxicity against the DU-145 tumor cell line (GI50 = 36 nM) and significantly disrupts the tumor vascular system. Its prodrug design enhances its bioavailability and delivery to tumor tissues.
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| Molecular Formula |
C26H26NO10P
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|---|---|
| Molecular Weight |
543.46
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| Exact Mass |
587.093
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| CAS # |
288847-41-6
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| PubChem CID |
9873180
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| Appearance |
Off-white to light yellow solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
40
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| Complexity |
815
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GQIZTUAJGVBAFG-UHFFFAOYSA-L
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| InChi Code |
InChI=1S/C26H26NO10P.2Na/c1-32-16-7-8-17-18(13-16)27-24(14-6-9-19(33-2)20(10-14)37-38(29,30)31)23(17)25(28)15-11-21(34-3)26(36-5)22(12-15)35-4;;/h6-13,27H,1-5H3,(H2,29,30,31);;/q;2*+1/p-2
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| Chemical Name |
disodium;[2-methoxy-5-[6-methoxy-3-(3,4,5-trimethoxybenzoyl)-1H-indol-2-yl]phenyl] phosphate
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| Synonyms |
OXi 8007; OXi-8007; OXi8007
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~90 mg/mL (~153.21 mM)
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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 | 1.8401 mL | 9.2003 mL | 18.4006 mL | |
| 5 mM | 0.3680 mL | 1.8401 mL | 3.6801 mL | |
| 10 mM | 0.1840 mL | 0.9200 mL | 1.8401 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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