1088715-84-7，LY2510924是有效，选择性的CXCR4拮抗剂

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号：1088715-84-7

分子式：C62H88N14O10

分子量：1189.450

结构式：

质量：1188.680786

密度：1.3±0.1 g/cm3

LogP：0.58

折射率：1.641

描述：LY2510924是有效，选择性的CXCR4拮抗剂；阻止SDF-1结合CXCR4的IC50值为0.079 nM。

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

陕西新研博美生物科技有限公司激酶实验：LY2510924特异性阻断SDF-1与CXCR4的结合，IC50值为0.079 nM，并抑制SDF-1诱导的GTP结合，Kb值为0.38 nM。在表达内源性CXCR4的人淋巴瘤U937细胞中，LY2510924抑制SDF-1诱导的细胞迁移，IC50值为0.26nM，并抑制SDF-1 / CXCR4介导的细胞内信号传导。 LY2510924在肿瘤细胞中表现出对SDF-1刺激的磷酸-ERK和磷酸-Akt的浓度依赖性抑制。生化和细胞分析显示LY2510924没有明显的激动剂活性[1]。 LY2510924主要抑制AML细胞的增殖，几乎不会诱导细胞死亡，并减少基质细胞对化疗的保护作用[2]。

[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

 以上信息均由陕西新研博美生物科技有限公司提供技术支持