GNE-2861
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
| Packaging | Price | Availability | Purity | Estimated Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry |
| Synonyms | GNE-2861; GNE 2861; GNE2861. |
|---|---|
| Molecular Formula | C22H26N6O2 |
| Molecular Weight | 406.48 |
| Appearance | Off-white solid to white solid |
| Purity | 98% Min. |
| Solubility | Soluble in DMSO, not in water |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shipping Condition | Shipped under ambient temperature |
| 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) |
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.
