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JB170

Chemical Structure : JB170

CAS No.: 2705844-82-0

JB170 (JB-170)

Catalog No.: PC-24082Not For Human Use, Lab Use Only.

JB170 is a potent, highly selective PROTAC degrader of Aurora A with DC50 of 28 nM and Dmax of 300 nM in MV4-11 cells, linking alisertib to the cereblon-binding molecule Thalidomide.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

JB170 is a potent, highly selective PROTAC degrader of Aurora A with DC50 of 28 nM and Dmax of 300 nM in MV4-11 cells, linking alisertib to the cereblon-binding molecule Thalidomide.
JB170 selectively binds AURORA-A (EC50=193 nM) over AURORA-B (EC50=1.4 µM).
JB170 reduces AURORA-A levels by inducing proteolysis, induces AURORA-A ubiquitylation by CEREBLON followed by proteolysis via the proteasome.
JB170 induces S-phase arrest in  in MV4-11 cells, induces apoptosis in cancer cells.

Physicochemical Properties

M.Wt 963.37
Formula C48H44ClFN8O11
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-((9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-benzo[c]pyrimido[4,5-e]azepin-2-yl)amino)-N-(2-(2-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetamido)ethoxy)ethoxy)ethyl)-2-methoxybenzamide

References

1. Adhikari B, et al. Nat Chem Biol. 2020;16(11):1179-1188.

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