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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

Molecular Formula : C22H26N6O2

Molecular Weight : 406.48

Iupac Chemical Name : 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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SynonymsGNE-2861; GNE 2861; GNE2861.
Molecular FormulaC22H26N6O2
Molecular Weight406.48
AppearanceOff-white solid to white solid
Purity98% Min.
SolubilitySoluble in DMSO, not in water
StorageDry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shipping ConditionShipped under ambient temperature 
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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