| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
Purity: ≥98%
ABT-510 acetate, the acetate salt form of ABT-510 which is a TSP-1 mimetic drug, is novel, potent and synthetic peptide consisting of nine-amino acids,it mimicks the anti-angiogenic activity of the endogenous protein thrombospondin-1 (TSP-1). ABT-510 inhibits the actions of several pro-angiogenic growth factors important to tumor neovascularization; these pro-angiogenic growth factors include vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF)), hepatocyte growth factor (HGF), and interleukin 8 (IL-8). ABT-510 was designed with TSRs as base, displayed anti-angiogenic properties in a phase 1 clinical trial in newly diagnosed glioblastoma.
| ln Vitro |
Inducing tolerance in ID 8 cells, ABT-510 acetate (1, 5, 10, 20, 50 nM; 24 h) raises the incidence of KS in the human epithelial cancer cell lines SKOV3, OVCAR3, and CAOV3 [1]. The development and height of NO-stimulated vascular cells into the extracellular matrix were reduced by acetate (0-10 μM; 7 days). ABT-510 acetate has the ability to stimulate CD36-mediated proliferation, NO-driven cGMP, and tumor-driven vascular cell growth [3].
|
|---|---|
| ln Vivo |
In mice, ABT-510 acetate (100 mg/kg; i.p.; once daily for 90 days) significantly reduces the size of epithelial cells, the volume of tumor ascites, and the spread of secondary tumors [1]. In models of inflammatory bowel illness, ABT-510 acetate (60 mg/kg; subcutaneous osmotic minipump; once daily for 7 days) decreases angiogenesis and inflammation [2].
|
| Cell Assay |
Apoptosis analysis [1]
Cell Types: ID8, SKOV3, OVCAR3 and CAOV3 cells Tested Concentrations: 1, 5, 10, 20, 50 nM Incubation Duration: 24 hrs (hours) Experimental Results: Induction of ID8 cell apoptosis and increased adsorption. Apoptosis in human EOC cell lines SKOV3, OVCAR3, and CAOV3. Cell proliferation assay[3] Cell Types: Tissue biopsy of B16F10 melanoma tumors grown in C57BL/6 mice Tested Concentrations: 0-10 μM Incubation Duration: 7 days Experimental Results: Inhibition of NO-stimulated vascular cell growth and invasion into the extracellular matrix . |
| Animal Protocol |
Animal/Disease Models: TSP-1-Null mouse (C57BL/6 background; orthotopic, syngeneic model of epithelial ovarian cancer) [1]
Doses: 100 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day for 90 days Experimental Results: diminished ovarian tumor growth in wild-type and TSP-1 null mice. The amount of ascites is Dramatically diminished and the formation of peritoneal lesions is completely eliminated. Reversal of ovarian tumor hypervascularization and increased proportion of mature vessels. Animal/Disease Models: TSP-1-Null mice (C57BL/6 background; 6 weeks old; DSS-induced inflammatory bowel disease mouse model) [2] Doses: 60 mg/kg Route of Administration: subcutaneously (sc) (sc) implanted osmotic minipump (0.5 µL/h) ); one time/day for 7 days Experimental Results: Dramatically delayed DSS-induced bleeding and improved overall disease severity. Inflammation grade and angiogenesis were Dramatically diminished. |
| References |
[1]. Greenaway J, et.al. ABT-510 induces tumor cell apoptosis and inhibits ovarian tumor growth in an orthotopic, syngeneic model of epithelial ovarian cancer. Mol Cancer Ther. 2009 Jan;8(1):64-74.
[2]. Punekar S,et.al. Thrombospondin 1 and its mimetic peptide ABT-510 decrease angiogenesis and inflammation in a murine model of inflammatory bowel disease. Pathobiology. 2008;75(1):9-21. [3]. Isenberg JS, et.al. Differential effects of ABT-510 and a CD36-binding peptide derived from the type 1 repeats of thrombospondin-1 on fatty acid uptake, nitric oxide signaling, and caspase activation in vascular cells. Biochem Pharmacol. 2008 Feb 15;75(4):875-82. |
| Molecular Formula |
C48H87N13O13
|
|---|---|
| Molecular Weight |
1054.28
|
| CAS # |
442526-87-6
|
| Related CAS # |
ABT-510;251579-55-2
|
| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
| SMILES |
O=C([C@H]1N(C([C@H](CCCNC(N)=N)NC([C@H]([C@@H](C)CC)NC([C@H](CCC)NC([C@H]([C@@H](O)C)NC([C@@H]([C@@H](C)CC)NC([C@H](C(C)C)NC(CNC(CN(C)C(C)=O)=O)=O)=O)=O)=O)=O)=O)=O)CCC1)NCC
|
| Chemical Name |
(S)-1-((2S,5S,8S,11S,14R,17S)-5,14-di((S)-sec-butyl)-2-(3-guanidinopropyl)-11-((S)-1-hydroxyethyl)-17-isopropyl-24-methyl-4,7,10,13,16,19,22,25-octaoxo-8-propyl-3,6,9,12,15,18,21,24-octaazahexacosan-1-oyl)-N-ethylpyrrolidine-2-carboxamide
|
| Synonyms |
ABT510 acetate ABT 510 ABT-510
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
H2O : ~100 mg/mL (~94.85 mM)
|
|---|---|
| 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 | 0.9485 mL | 4.7426 mL | 9.4851 mL | |
| 5 mM | 0.1897 mL | 0.9485 mL | 1.8970 mL | |
| 10 mM | 0.0949 mL | 0.4743 mL | 0.9485 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA