ChemicalBook--->CAS DataBase List--->442526-87-6

442526-87-6

442526-87-6 Structure

442526-87-6 Structure
IdentificationBack Directory
[Name]

L-Prolinamide, N-acetyl-N-methylglycylglycyl-L-valyl-D-alloisoleucyl-L-threonyl-L-norvalyl-L-isoleucyl-L-arginyl-N-ethyl-, monoacetate (salt) (9CI)
[CAS]

442526-87-6
[Synonyms]

ABT510 acetate
ABT-510 acetate
ABT 510 acetate
L-Prolinamide, N-acetyl-N-methylglycylglycyl-L-valyl-D-alloisoleucyl-L-threonyl-L-norvalyl-L-isoleucyl-L-arginyl-N-ethyl-, monoacetate (salt) (9CI)
[Molecular Formula]

C48H87N13O13
[MOL File]

442526-87-6.mol
[Molecular Weight]

1054.3
Chemical PropertiesBack Directory
[form ]

Solid
[color ]

White to off-white
[Sequence]

Ac-{Sar}-Gly-Val-{DalloIle}-Thr-{Nva}-Ile-Arg-{Pro-NHEt}
Hazard InformationBack Directory
[Uses]

ABT-510 acetate is an anti-angiogenic TSP peptide (Thrombospondin-1 analogue) that induces apoptosis and inhibits ovarian tumour growth in an orthotopic, syngeneic model of epithelial ovarian cancer. ABT-510 acetate also reduces angiogenesis and inflammatory responses in a murine model of inflammatory bowel disease. ABT-510 acetate can be used in studies of cancer (particularly epithelial ovarian cancer) and inflammatory bowel disease (IBD)[1][2].
[in vivo]

ABT-510 acetate (100 mg/kg; i.p.; single daily for 90 days) induces cells apoptosisin vivo and leads to a significant reduction in epithelial ovarian tumor size, ascites fluid volume, and secondary lesion dissemination in mice[1].
ABT-510 acetate (60 mg/kg; osmotic minipumps for s.c.; single daily for 7 days) decreases angiogenesis and inflammation in a murine model of inflammatory bowel disease[2].

Animal Model:TSP-1-Null mice (C57BL/6 background; orthotopic, syngeneic model of epithelial ovarian cancer)[1]
Dosage:100 mg/kg
Administration:Intraperitoneal injection; single daily for 90 days
Result:Reduced ovarian tumor growth in wild-type and TSP-1-Null Mice.
Significantly reduced the volume of ascites and completely abolished the formation of peritoneal lesions.
Reversed ovarian tumor hypervascularization and increased the proportion of mature blood vessels.
Animal Model:TSP-1-Null mice (C57BL/6 background; 6-week-old; DSS-induced inflammatory bowel disease murine model)[2]
Dosage:60 mg/kg
Administration:Subcutaneously implanted osmotic minipumps (0.5μL/h); single daily for 7 days
Result:Significantly delayed DSS-induced bleeding and improved the overall severity of disease.
Significantly diminished inflammation grading and angiogenesis.
[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. DOI:10.1158/1535-7163.MCT-08-0864
[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. DOI:10.1159/000113790
[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. DOI:10.1016/j.bcp.2007.10.025
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