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ZZ151

Chemical Structure : ZZ151

CAS No.: 2920192-97-6

ZZ151 (ZZ-151)

Catalog No.: PC-20168Not For Human Use, Lab Use Only.

ZZ151 (ZZ-151) is a highly potent and selective SOS1 degrader PROTAC with DC50 of 15.7 nM (Dmax=100%).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

ZZ151 (ZZ-151) is a highly potent and selective SOS1 degrader PROTAC with DC50 of 15.7 nM (Dmax=100%).
ZZ151 induces SOS1 degradation via the VHL-dependent proteasomal degradation pathway.
ZZ151 potently, specifically and quickly induces SOS1 degradation.
ZZ151 potently induces SOS1 degradation in cells harboring KRAS mutations of G12C, G12D, G12V, G12R, G12S, and G13D with DC50 values ranged from 8.41 to 41.4 nM.
ZZ151 (20 mg/kg) significantly inhibits the tumor growth of KRASG12D- and KRASG12V-mutant xenografts in mice, with no body weight loss.

Physicochemical Properties

M.Wt 1028.25
Formula C54H68F3N9O6S
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

(2S,4R)-1-((S)-2-(7-(4-(4-(((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)amino)-7-methoxy-2-methylquinazolin-6-yl)piperidin-1-yl)-7-oxoheptanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide

References

1. Zehui Zhou, et al. J Med Chem. 2023 Mar 10. doi: 10.1021/acs.jmedchem.3c00075.

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