021-51111890
购物车（0）
sales@molnova.cn
LY-2510924
CAS No. 1088715-84-7
LY-2510924 ( LY2510924 )
产品货号. M10339 CAS No. 1088715-84-7
LY-2510924 (LY2510924) 是一种有效的选择性环肽 CXCR4 拮抗剂，IC50 为 0.079 nM。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 25MG | ￥6456 | 有现货 |
|
| 50MG | ￥10368 | 有现货 |
|
| 100MG | ￥15714 | 有现货 |
|
| 200MG | 获取报价 | 有现货 |
|
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
-
产品名称LY-2510924
-
注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
-
产品简述LY-2510924 (LY2510924) 是一种有效的选择性环肽 CXCR4 拮抗剂，IC50 为 0.079 nM。
-
产品描述LY-2510924 (LY2510924)?is a potent and selective, cyclic peptide CXCR4 antagonist with IC50 of 0.079 nM, without apparent agonist activity; inhibits SDF-1-induced cell migration with IC50 of 0.26 nM and inhibits SDF-1/CXCR4-mediated intracellular signaling; exhibits inhibition of SDF-1-stimulated phospho-ERK and phospho-Akt in tumor cells; shows inhibition of tumor growth in human xenograft models with acceptable in vivo stability and a pharmacokinetic profile.Kidney Cancer Phase 2 Clinical.
-
体外实验LY2510924 specifically blocks SDF-1 binding to CXCR4 with IC50 value of 0.079 nM, and inhibits SDF-1–induced GTP binding with Kb value of 0.38 nM. In human lymphoma U937 cells expressing endogenous CXCR4, LY2510924 inhibits SDF-1–induced cell migration with IC50 value of 0.26 nM and inhibits SDF-1/CXCR4-mediated intracellular signaling. LY2510924 exhibits a concentration-dependent inhibition of SDF-1–stimulated phospho-ERK and phospho-Akt in tumor cells. Biochemical and cellular analyses reveals that LY2510924 has no apparent agonist activity. LY2510924 chiefly inhibits the proliferation of AML cells with little induction of cell death and reduces protection against chemotherapy by stromal cells.
-
体内实验LY2510924 specifically blocks SDF-1 binding to CXCR4 with IC50 value of 0.079 nM, and inhibits SDF-1–induced GTP binding with Kb value of 0.38 nM. In human lymphoma U937 cells expressing endogenous CXCR4, LY2510924 inhibits SDF-1–induced cell migration with IC50 value of 0.26 nM and inhibits SDF-1/CXCR4-mediated intracellular signaling. LY2510924 exhibits a concentration-dependent inhibition of SDF-1–stimulated phospho-ERK and phospho-Akt in tumor cells. Biochemical and cellular analyses reveals that LY2510924 has no apparent agonist activity. LY2510924 chiefly inhibits the proliferation of AML cells with little induction of cell death and reduces protection against chemotherapy by stromal cells.
-
同义词LY2510924
-
通路GPCR/G Protein
-
靶点Chemokine Receptor
-
受体Chemokine Receptor
-
研究领域Cancer
-
适应症Kidney Cancer
化学信息
-
CAS Number1088715-84-7
-
分子量1189.45
-
分子式C62H88N14O10
-
纯度>98% (HPLC)
-
溶解度DMSO : ≥ 125 mg/mL105.09 mM
-
SMILESO=C(NCC(N[C@@H](C(N[C@@H](CCCCNC(C)C)C(N)=O)=O)CCC(N[C@@H](CC1=CC=CC=C1)C(N[C@@H](CC2=CC=C(O)C=C2)C3=O)=O)=O)=O)C(CC4=CC=C(C=CC=C5)C5=C4)NC(C(CCCNC(N)=O)NC(C(N3)CCCCNC(C)C)=O)=O
-
化学全称Cyclo[Phe-Tyr-Lys(iPr)-D-Arg-2-Nal-Gly-D-Glu]-Lys(iPr)-NH2
运输与储存
-
储存条件(-20℃)
-
运输条件With Ice Pack
-
稳定性≥ 2 years
参考文献
1. Peng SB, et al. Mol Cancer Ther. 2015 Feb;14(2):480-90.
2. Cho BS, et al. Blood. 2015 Jul 9;126(2):222-32.
3. Galsky MD, et al. Cancer Res. 2014 Aug 15;20(16):4414.
