GSK923295 (GSK-923295A)

Alias: GSK923295; GSK-923295A; GSK 923295; GSK923295A;GSK-923295; GSK 923295A.
Cat No.:V1629 Purity: ≥98%
GSK923295 (also called GSK-923295;GSK923295A;GSK 923295;GSK-923295A) is a first-in-class, specific and allosteric antimitotic inhibitor of CENP-E (centromere-associated protein E, kinesin motor ATPase)with potential antitumor activity.
GSK923295 (GSK-923295A) Chemical Structure CAS No.: 1088965-37-0
Product category: Kinesin
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

GSK923295 (also called GSK-923295; GSK923295A; GSK 923295; GSK-923295A) is a first-in-class, specific and allosteric antimitotic inhibitor of CENP-E (centromere-associated protein E, kinesin motor ATPase) with potential antitumor activity. It inhibits CENP-E with a Ki of 3.2 nM, and it is less potent against mutant I182 and T183. GSK923295A has demonstrated high antitumor activity against various solid tumor models such as CRs in rhabdoid, Ewing sarcoma, and rhabdomyosarcoma xenografts.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
GSK-923295 (GSK923295) is an allosteric inhibitor of CENP-E kinesin motor activity that is unique in its class. With a Ki of 3.2± 0.2 nM for humans and 1.6±0.1 nM for dogs, GSK923295 inhibits CENP-E MT-stimulated ATPase activity without being competitive with either ATP or MT. Inorganic phosphate release is inhibited by GSK923295, and CENP-E motor domain association with microtubules is stabilized[1]. IC50s for GSK923295's broad growth inhibitory activity in a panel of 237 cancer cell lines are 17.2 nM, 55.6 nM, 42 nM, and 51.9 nM for SW48, RKO (BRAF mutant), SW620 (KRAS mutant), and HCT116 (KRAS mutant), respectively. Eight of the eleven mouse xenograft tumor models exhibit significant tumor growth-delay[2]. With a Ki of 3.2 nM, GSK923295 is a strong and specific small molecule inhibitor of human CENPE. With an average growth IC50 of 41 nM, GSK923295 exhibits broad effectiveness against a panel of 19 human neuroblastoma derived cell lines[3].
ln Vivo
In comparison to the control arm, the xenografts of mice treated with GSK-923295 (GSK923295) exhibit a significant delay in tumor growth (NB-EBc1 p<0.0001; NB-1643 p=0.018; NB-1691 p=0.0018)[3].
Animal Protocol
Dissolved in 4% N,N-dimethylacetamide (DMA)/Cremaphore (50/50) at pH 5.6; 125 mg/kg; i.p. injection
Mice bearing xenografts of the Colo205 colon tumor-cell line
References
[1]. Wood KW, et al. Antitumor activity of an allosteric inhibitor of centromere-associated protein-E. Proc Natl Acad Sci U S A. 2010 Mar 30;107(13):5839-44.
[2]. Mayes PA, et al. Mitogen-activated protein kinase (MEK/ERK) inhibition sensitizes cancer cells to centromere-associated protein E (CENP-E) inhibition. Int J Cancer. 2013 Feb 1;132(3):E149-57.
[3]. Balamuth NJ, et al. Serial transcriptome analysis and cross-species integration identifies centromere-associated protein E as a novel neuroblastoma target. Cancer Res. 2010 Apr 1;70(7):2749-58
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C32H38CLN5O4
Molecular Weight
592.13
CAS #
1088965-37-0
SMILES
O=C(N[C@@H](CC1=CC=C(C2=CN3C=CC=C([C@@H](O)C)C3=N2)C=C1)CNC(CN(C)C)=O)C4=CC=C(OC(C)C)C(Cl)=C4
Synonyms
GSK923295; GSK-923295A; GSK 923295; GSK923295A;GSK-923295; GSK 923295A.
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 100 mg/mL (168.9 mM)
Water:<1 mg/mL
Ethanol:100 mg/mL (168.9 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.6888 mL 8.4441 mL 16.8882 mL
5 mM 0.3378 mL 1.6888 mL 3.3776 mL
10 mM 0.1689 mL 0.8444 mL 1.6888 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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Biological Data
  • GSK923295

    GSK923295 inhibits microtubule (MT)-stimulated ATPase of CENP-E and promotes formation of a MT-bound complex. Proc Natl Acad Sci U S A. 2010 Mar 30;107(13):5839-44.
  • GSK923295

    Proc Natl Acad Sci U S A. 2010 Mar 30;107(13):5839-44. Antitumor activity of GSK923295.
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