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.
For research use only. We do not sell to patients.
Chemical Information
| Name | GNE-2861 |
|---|---|
| Iupac Chemical Name | 1-(2-(1-(2-aminopyrimidin-4-yl)-2-((2-methoxyethyl)amino)-1H-1,3-benzodiazol-6-yl)ethynyl)cyclohexan-1-ol |
| Synonyms | GNE-2861; GNE 2861; GNE2861. |
| Molecular Formula | C22H26N6O2 |
| Molecular Weight | 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 Number | 1394121-05-1 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Off-white solid to white solid |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO, not in water |
| Handling | |
| Shipping Condition | Shipped under ambient temperature |
| HS Code |
| Targets | |
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| 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.
Chemical Structure
