GNE-2861
GNE-2861 is a potent and exquisitely kinase-selective Group II PAK inhibitor (PAK4 Ki = 3 nM). GNE-2861 sensitized tamoxifen resistant MCF-7/LCC2 breast cancer cells to tamoxifen. PAK4 is overexpressed and/or genetically amplified in lung, colon, prostate, pancreas, and breast cancer cell lines and tumor tissues.
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化学信息
| 名称 | GNE-2861 |
|---|---|
| Iupac 化学名称 | 1-(2-(1-(2-aminopyrimidin-4-yl)-2-((2-methoxyethyl)amino)-1H-1,3-benzodiazol-6-yl)ethynyl)cyclohexan-1-ol |
| 同义词 | GNE-2861; GNE 2861; GNE2861. |
| 英文同义词 | GNE-2861; GNE 2861; GNE2861. |
| 分子式 | C22H26N6O2 |
| 分子量 | 406.48 |
| Smile | NC1=NC=CC(=N1)N1C(=NC2=C1C=C(C=C2)C#CC2(CCCCC2)O)NCCOC |
| InChiKey | RZXMIHOUHYSGJO-UHFFFAOYSA-N |
| InChi | InChI=1S/C22H26N6O2/c1-30-14-13-25-21-26-17-6-5-16(7-11-22(29)9-3-2-4-10-22)15-18(17)28(21)19-8-12-24-20(23)27-19/h5-6,8,12,15,29H,2-4,9-10,13-14H2,1H3,(H,25,26)(H2,23,24,27) |
| Cas号 | 1394121-05-1 |
| 相关CAS号 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 类白色至白色固体 |
|---|---|
| 纯度 | 98% Min. |
| 存储 | 短期可在0-4度保存，数天至数月；长期可在-20度保存三年。 |
| 可溶性 | 可溶于DMSO；不溶于水 |
| 处理方式 | |
| 运输条件 | 可在常温下运输 |
| 海关编码 |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Zhuang T, Zhu J, Li Z, Lorent J, Zhao C, Dahlman-Wright K, Strömblad S.
p21-activated kinase group II small compound inhibitor GNE-2861 perturbs estrogen
receptor alpha signaling and restores tamoxifen-sensitivity in breast cancer
cells. Oncotarget. 2015 Dec 22;6(41):43853-68. doi: 10.18632/oncotarget.6081.
PubMed PMID: 26554417; PubMed Central PMCID: PMC4791272.
2: Staben ST, Feng JA, Lyle K, Belvin M, Boggs J, Burch JD, Chua CC, Cui H,
DiPasquale AG, Friedman LS, Heise C, Koeppen H, Kotey A, Mintzer R, Oh A, Roberts
DA, Rouge L, Rudolph J, Tam C, Wang W, Xiao Y, Young A, Zhang Y, Hoeflich KP.
Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity
for type I 1/2 kinase inhibitors. J Med Chem. 2014 Feb 13;57(3):1033-45. doi:
10.1021/jm401768t. Epub 2014 Feb 4. PubMed PMID: 24432870.
