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(hào)：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(diǎn)：SDF-1α-CXCR4:79.7 pM (IC50)；SDF-1α-CXCR4:49.5 pM (Ki)

激酶實(shí)驗(yàn)：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(hào)傳導(dǎo)。 LY2510924在腫瘤細(xì)胞中表現(xiàn)出對(duì)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(dòng)劑活性[1]。 LY2510924主要抑制AML細(xì)胞的增殖，幾乎不會(huì)誘導(dǎo)細(xì)胞死亡，并減少基質(zhì)細(xì)胞保護(hù)作用[2]。

動(dòng)物實(shí)驗(yàn)：

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(dòng)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(dòng)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(shí)，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.

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LY2510924 1088715-84-7

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CTTHWGFTLC, CYCLIC 244082-19-7

1088715-84-7，LY2510924螯合劑