ChemicalBook CAS DataBase List 442526-87-6

442526-87-6

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
Molecular Formula	C48H87N13O13
Molecular Weight	1054.3
MOL File	442526-87-6.mol

Chemical Properties

form	Solid
color	White to off-white
Sequence	Ac-{Sar}-Gly-Val-{DalloIle}-Thr-{Nva}-Ile-Arg-{Pro-NHEt}

Hazard Information

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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