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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 & Documentation
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.

Chemical Information
Molecular Weight 592.13
Formula C32H38ClN5O4
CAS Number 1088965-37-0
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

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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Keywords: GSK923295 supplier, Kinesin, inhibitors, activators


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