詳細(xì)介紹
1088715-84-7,LY2510924螯合劑
英文名:LY2510924
1,4,7,10,13,16,19-Heptaazacyclotricosane-20-carboxamide, N-[(1S)-1-(aminocarbonyl)-5-[(1-methylethyl)amino]pentyl]-11-[3-[(aminoiminomethyl)amino]propyl]-5-[(4-hydroxyphenyl)methyl]-8-[4-[(1-methylethyl)amino]butyl]-14-(2-naphthalenylmethyl)-3,6,9,12,15,18,23-heptaoxo-2-(phenylmethyl)-, (2S,5S,8S,11R,14S,20R)-
(2S,5S,8S,11R,14S,20R)-N-[(2S)-1-Amino-6-(isopropylamino)-1-oxo-2-hexanyl]-2-benzyl-11-(3-carbamimidamidopropyl)-5-(4-hydroxybenzyl)-8-[4-(isopropylamino)butyl]-14-(2-naphthylmethyl)-3,6,9,12,15,18,23-heptaoxo-1,4,7,10,13,16,19-heptaazacyclotricosane-20-carboxamide
CAS號:1088715-84-7
分子式:C62H88N14O10
分子量:1189.450
結(jié)構(gòu)式:
***質(zhì)量:1188.680786
密度:1.3±0.1 g/cm3
LogP:0.58
折射率:1.641
描述:LY2510924是有效,選擇性的CXCR4拮抗劑;阻止SDF-1結(jié)合CXCR4的IC50值為0.079 nM。
靶點:SDF-1α-CXCR4:79.7 pM (IC50);SDF-1α-CXCR4:49.5 pM (Ki)
激酶實驗:LY2510924特異性阻斷SDF-1與CXCR4的結(jié)合,IC50值為0.079 nM,并抑制SDF-1誘導(dǎo)的GTP結(jié)合,Kb值為0.38 nM。在表達(dá)內(nèi)源性CXCR4的人淋巴瘤U937細(xì)胞中,LY2510924抑制SDF-1誘導(dǎo)的細(xì)胞遷移,IC50值為0.26nM,并抑制SDF-1 / CXCR4介導(dǎo)的細(xì)胞內(nèi)信號傳導(dǎo)。 LY2510924在腫瘤細(xì)胞中表現(xiàn)出對SDF-1刺激的磷酸-ERK和磷酸-Akt的濃度依賴性抑制。生化和細(xì)胞分析顯示LY2510924沒有明顯的激動劑活性[1]。 LY2510924主要抑制AML細(xì)胞的增殖,幾乎不會誘導(dǎo)細(xì)胞死亡,并減少基質(zhì)細(xì)胞保護作用[2]。
動物實驗:
小鼠:SCID雌性小鼠靜脈內(nèi)注射MDA-MB-231細(xì)胞,并用載體(1×PBS)或3mg / kg配制在1×PBS中的LY2510924皮下處理。***組和第2組動物每天兩次接受載體或3mg / kg LY2510924,持續(xù)數(shù)天,在腫瘤細(xì)胞注射***天開始***。第3組動物每天兩次接受3mg / kg LY2510924 15,持續(xù)13天,在腫瘤細(xì)胞注射后一天開始***。***后,肺組織在10%中性緩沖福爾馬林中固定至少24小時,肺葉存在于組織切片[1]。
參考文獻(xiàn):
[1]. Peng SB, et al. Identification of LY2510924, a novel cyclic peptide CXCR4 antagonist that exhibits antitumor activities in solid tumor and breast cancer metastatic models. Mol Cancer Ther. 2015 Feb;14(2):480-90.
[2]. Cho BS, et al. Antileukemia activity of the novel peptidic CXCR4 antagonist LY2510924 as monotherapy and in combination with chemotherapy. Blood. 2015 Jul 9;126(2):222-32.
其它產(chǎn)品列表:
c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-d-Arg-NEt2 acetate 1647120-04-4
Cyclo(-Trp-Pro) 38136-70-8
Cyclo(D-Leu-L-Pro) 36238-67-2
Cyclo(-Gly-Tyr) 5845-66-9
Cyclo(-D-Ser-Pro-D-Val-Leu-D-Trp) 153982-38-8
Cyclo(-Gly-Arg-Gly-Asp-Ser-Pro-Ala) 128857-77-2
Cyclo(-Tyr-Hpro) 813461-21-1
Cyclo-(D-Tyr-Gly) 1217777-38-2
Cyclo(-Ala-Tyr) 21754-26-7
LY2510924 1088715-84-7
Cyclo(-Tyr-Arg) 81205-31-4
Cyclo(D-Tyr-D-Phe)
Cyclo(L-Phe-trans-4-hydroxy-L-Pro) 118477-06-8
Cyclo(-Gly-Asn-Trp-His-Gly-Thr-Ala-Pro-Asp)-Trp-Val-Tyr-Phe-Ala-His-Leu-Asp-Ile-Ile-Trp-OH 151308-48-4
Cyclo(L-Leu-trans-4-hydroxy-L-Pro) 115006-86-5
(Cyclo(Glu22-Lys26),Leu27)-pTH (1-31) amide (human) 188899-65-2
Cyclo(Hpro-Leu) 1016899-93-6
Cyclo(-Hyp-Gly)
Cyclo-Somatostatin acetate salt 84211-54-1
CTTHWGFTLC, CYCLIC 244082-19-7
1088715-84-7,LY2510924螯合劑