GSK 923295A

Pricing Availability   Qty
Description: Potent and selective centromere associated protein E (CENP-E) allosteric inhibitor
Chemical Name: 3-Chloro-N-[(1S)-2-[[2-(dimethylamino)acetyl]amino]-1-[[4-[8-[(1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl]phenyl]methyl]ethyl]-4-(1-methylethoxy)benzamide
Purity: ≥97% (HPLC)
Literature (2)

Biological Activity for GSK 923295A

GSK 923295A is a potent and selective centromere associated protein E (CENP-E) allosteric inhibitor (IC50 = 22 nM); does not compete with ATP. Exhibits selectivity over a panel of other kinesins (<25% inhibition at 50 μM). Inhibits tumor cell growth in vitro. Induces mitotic arrest and regression of human tumor xenografts in vivo.

Technical Data for GSK 923295A

M. Wt 592.13
Formula C32H38ClN5O4
Storage Store at -20°C
Purity ≥97% (HPLC)
CAS Number 1088965-37-0
PubChem ID 46898058
Smiles CC(OC1=C(C=C(C(N[C@@H](CC2=CC=C(C3=CN4C=CC=C(C4=N3)[C@@H](O)C)C=C2)CNC(CN(C)C)=O)=O)C=C1)Cl)C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for GSK 923295A

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 59.21 100
ethanol 11.84 20 with gentle warming

Preparing Stock Solutions for GSK 923295A

The following data is based on the product molecular weight 592.13. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.69 mL 8.44 mL 16.89 mL
5 mM 0.34 mL 1.69 mL 3.38 mL
10 mM 0.17 mL 0.84 mL 1.69 mL
50 mM 0.03 mL 0.17 mL 0.34 mL

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References for GSK 923295A

References are publications that support the biological activity of the product.

Qian et al (2010) Discovery of the first potent and selective inhibitor of centromere-associated protein E: GSK923295. ACS Med.Chem.Lett. 1 30 PMID: 24900171

Wood et al (2010) Antitumor activity of an allosteric inhibitor of centromere-associated protein-E. Proc.Natl.Acad.Sci.U.S.A. 107 5839 PMID: 20167803

If you know of a relevant reference for GSK 923295A, please let us know.

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Keywords: GSK 923295A, GSK 923295A supplier, GSK923295A, ATPase, Potent, selective, centromere, associated, protein, E, CENP-E, allosteric, inhibitors, inhibits, mitotic, kinesin, mitosis, Kinesin, 6837, Tocris Bioscience

Citations for GSK 923295A

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