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GNE-2861

Catalog No.: 111892
Cas No.: 1394121-05-1
Purity : 98% Min.
111892 - GNE-2861 | CAS 1394121-05-1

Catalog number : 111892

CAS number : 1394121-05-1

分子式 : C22H26N6O2

分子量 : 406.48

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

Smile : NC1=NC=CC(=N1)N1C(=NC2=C1C=C(C=C2)C#CC2(CCCCC2)O)NCCOC

InChiKey : RZXMIHOUHYSGJO-UHFFFAOYSA-N

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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
外观 类白色至白色固体
纯度98% Min.
可溶性可溶于DMSO;不溶于水
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。
运输条件可在常温下运输
SmileNC1=NC=CC(=N1)N1C(=NC2=C1C=C(C=C2)C#CC2(CCCCC2)O)NCCOC
InChiKeyRZXMIHOUHYSGJO-UHFFFAOYSA-N
InChiInChI=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)
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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.

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.


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