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GSK923295

Cat. No. M2171
GSK923295 Structure
Size Price Availability Quantity
5mg USD 115  USD115 In stock
10mg USD 190  USD190 In stock
50mg USD 660  USD660 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

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

[1] Mayes PA, et al. Int J Cancer. Mitogen-activated protein kinase (MEK/ERK) inhibition sensitizes cancer cells to centromere-associated protein E inhibition.

[2] Lock RB, et al. Pediatr Blood Cancer. Initial testing of the CENP-E inhibitor GSK923295A by the pediatric preclinical testing program.

[3] Wood KW, et al. Proc Natl Acad Sci U S A. Antitumor activity of an allosteric inhibitor of centromere-associated protein-E.

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  Catalog
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Keywords: GSK923295 supplier, Kinesin, inhibitors

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