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251579-55-2
  • names:

    (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

  • CAS号:

    251579-55-2

    MDL Number:
  • MF(分子式): C46H83N13O11 MW(分子量): 994.23
  • EINECS: Reaxys Number:
  • Pubchem ID: Brand:BIOFOUNT
ABT-510
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中文别名 ABT-510
英文别名 ABT510; ABT 510; ABT-510
CAS号 251579-55-2
Inchi InChI=1S/C46H83N13O11/c1-12-18-30(39(64)55-36(26(7)13-2)42(67)53-31(19-16-21-50-46(47)48)45(70)59-22-17-20-32(59)40(65)49-15-4)52-44(69)38(28(9)60)57-43(68)37(27(8)14-3)56-41(66)35(25(5)6)54-33(62)23-51-34(63)24-58(11)29(10)61/h25-28,30-32,35-38,60H,12-24H2,1-11H3,(H,49,65)(H,51,63)(H,52,69)(H,53,67)(H,54,62)(H,55,64)(H,56,66)(H,57,68)(H4,47,48,50)/t26-,27-,28-,30-,31-,32-,35-,36-,37+,38-/m0/s1
InchiKey RIWLPSIAFBLILR-SYGZVSRYSA-N
分子式 Formula C46H83N13O11
分子量 Molecular Weight 994.23
溶解度Solubility
性状 Solid powder
储藏条件 Storage conditions Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).
产品说明 ABT-510(CAS:251579-55-2):仅限应用于工业或者科学研究过程中非医疗目的,不应用于人类或动物的临床诊断以及治过程疗,该产品非药用,非食用。
IntroductionABT-510 is synthetic peptide that mimics 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).
Application1
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[1]Campbell NE, Greenaway J, Henkin J, Moorehead RA, Petrik J. The thrombospondin-1 mimetic ABT-510 increases the uptake and effectiveness of cisplatin and paclitaxel in a mouse model of epithelial ovarian cancer. Neoplasia. 2010 Mar;12(3):275-83. PubMed PMID: 20234821; PubMed Central PMCID: PMC2838444.
[2]Nabors LB, Fiveash JB, Markert JM, Kekan MS, Gillespie GY, Huang Z, Johnson MJ, Meleth S, Kuo H, Gladson CL, Fathallah-Shaykh HM. A phase 1 trial of ABT-510 concurrent with standard chemoradiation for patients with newly diagnosed glioblastoma. Arch Neurol. 2010 Mar;67(3):313-9. PubMed PMID: 20212229.
[3] Tolle JC, Becker CL, Califano JC, Chang JL, Gernhardt K, Napier JJ, Wittenberger SJ, Yuan J. Impurity rejection in the crystallization of ABT-510 as a method to establish starting material specifications. Adv Exp Med Biol. 2009;611:595-6. PubMed PMID: 19400326.
[4] Becker CL, Califano JC, Tolle JC, Napier JJ, Kolaczkowski L, Chang SJ, Tian Z, Manna S. Evolution of the synthetic process to prepare the tripeptide segment of ABT-510. Adv Exp Med Biol. 2009;611:575-6. PubMed PMID: 19400320.
[5] Hasina R, Martin LE, Kasza K, Jones CL, Jalil A, Lingen MW. ABT-510 is an effective chemopreventive agent in the mouse 4-nitroquinoline 1-oxide model of oral carcinogenesis. Cancer Prev Res (Phila). 2009 Apr;2(4):385-93. Epub 2009 Mar 31. PubMed PMID: 19336725; PubMed Central PMCID: PMC2702843.
6: Greenaway J, Henkin J, Lawler J, Moorehead R, Petrik J. 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. PubMed PMID: 19139114.7: Baker LH, Rowinsky EK, Mendelson D, Humerickhouse RA, Knight RA, Qian J, Carr RA, Gordon GB, Demetri GD. Randomized, phase II study of the thrombospondin-1-mimetic angiogenesis inhibitor ABT-510 in patients with advanced soft tissue sarcoma. J Clin Oncol. 2008 Dec 1;26(34):5583-8. Epub 2008 Nov 3. PubMed PMID: 18981463.8: Gordon MS, Mendelson D, Carr R, Knight RA, Humerickhouse RA, Iannone M, Stopeck AT. A phase 1 trial of 2 dose schedules of ABT-510, an antiangiogenic, thrombospondin-1-mimetic peptide, in patients with advanced cancer. Cancer. 2008 Dec 15;113(12):3420-9. PubMed PMID: 18932258.9: Punekar S, Zak S, Kalter VG, Dobransky L, Punekar I, Lawler JW, Gutierrez LS. 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. Epub 2008 Mar 11. PubMed PMID: 18334835.10: Isenberg JS, Yu C, Roberts DD. 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. Epub 2007 Nov 1. PubMed PMID: 18068687; PubMed Central PMCID: PMC2267764.
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