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GSK923295

Cat. No. M2171
GSK923295 Structure
Size Price Availability Quantity
10mg USD 190 In stock
50mg USD 680 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

GSK923295 is a small-molecule inhibitor of the mitotic kinesin centromere-associated protein E (CENP-E). GSK923295 inhibited release of inorganic phosphate and stabilized CENP-E motor domain interaction with microtubules. GSK923295 demonstrated significant antitumor activity against solid tumor models, inducing CRs in Ewing sarcoma, rhabdoid, and rhabdomyosarcoma xenografts. GSK923295 exhibits robust, dose-dependent antitumor activity against Colo205 xenografts, including partial and complete regressions at the 125 mg/kg dose.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 592.13
Formula C32H38ClN5O4
CAS Number 1088965-37-0
Purity >98%
Solubility DMSO
Storage at -20°C
References

Mitogen-activated protein kinase (MEK/ERK) inhibition sensitizes cancer cells to centromere-associated protein E inhibition.
Mayes PA, et al. Int J Cancer. 2013 Feb 1;132(3):E149-57. PMID: 22948716.

Initial testing of the CENP-E inhibitor GSK923295A by the pediatric preclinical testing program.
Lock RB, et al. Pediatr Blood Cancer. 2012 Jun;58(6):916-23. PMID: 21584937.

Antitumor activity of an allosteric inhibitor of centromere-associated protein-E.
Wood KW, et al. Proc Natl Acad Sci U S A. 2010 Mar 30;107(13):5839-44. PMID: 20167803.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GSK923295 supplier, Kinesin, inhibitors

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