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SNIPER(ER)-87 

Cat. No. M29371
SNIPER(ER)-87  Structure
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Quality Control & Documentation
Biological Activity

SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen by a PEG linker, and efficiently degrades the ERα protein (IC50=0.097 μM). SNIPER(ER)-87 preferentially recruits XIAP to ERα in the cells, and XIAP is the primary E3 ubiquitin ligase responsible for the SNIPER(ER)-87-induced ERα degradation.

Chemical Information
Molecular Weight 1044.3
Formula C59H73N5O10S
CAS Number 2222354-91-6
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Nobumichi Ohoka, et al. J Biol Chem. Derivatization of inhibitor of apoptosis protein (IAP) ligands yields improved inducers of estrogen receptor α degradation

[2] Nobumichi Ohoka, et al. J Biol Chem. In Vivo Knockdown of Pathogenic Proteins via S pecific and N ongenetic I nhibitor of Apoptosis Protein (IAP)-dependent P rotein Er asers (SNIPERs)

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  Catalog
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Keywords: SNIPER(ER)-87  supplier, PROTAC, inhibitors, activators


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