GNE-2861
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MedKoo CAT#: 407863

CAS#: 1394121-05-1

Description: 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.


Price and Availability

Size Price Shipping out time Quantity
10mg USD 150 Same day
25mg USD 330 Same day
50mg USD 550 Same day
100mg USD 950 Same day
200mg USD 1650 Same day
Inquire bulk and customized quantity

Pricing updated 2020-10-31. Prices are subject to change without notice.

GNE-2861, purity > 98%, is in stock. The same day shipping out after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 407863
Name: GNE-2861
CAS#: 1394121-05-1
Chemical Formula: C22H26N6O2
Exact Mass: 406.2117
Molecular Weight: 406.49
Elemental Analysis: C, 65.01; H, 6.45; N, 20.68; O, 7.87


Synonym: GNE-2861; GNE 2861; GNE2861.

IUPAC/Chemical Name: 1-(2-(1-(2-aminopyrimidin-4-yl)-2-((2-methoxyethyl)amino)-1H-1,3-benzodiazol-6-yl)ethynyl)cyclohexan-1-ol

InChi Key: RZXMIHOUHYSGJO-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: OC1(C#CC2=CC=C3N=C(NCCOC)N(C4=NC(N)=NC=C4)C3=C2)CCCCC1


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (SDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
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

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


Additional Information

Estrogen receptor alpha (ERα) is highly expressed in most breast cancers. Consequently, ERα modulators, such as tamoxifen, are successful in breast cancer treatment, although tamoxifen resistance is commonly observed. While tamoxifen resistance may be caused by altered ERα signaling, the molecular mechanisms regulating ERα signaling and tamoxifen resistance are not entirely clear


References

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.