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SHP389

Chemical Structure : SHP389

CAS No.: 2235394-90-6

SHP389 (SHP-389;SHP 389)

Catalog No.: PC-36050Not For Human Use, Lab Use Only.

SHP389 (SHP-389, SHP 389) is a novel potent, selective, allosteric SHP2 inhibitor with IC50 of 36 nM, shows with impressive hERG selectivity (IC50>30 uM).

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Biological Activity

SHP389 (SHP-389, SHP 389) is a novel potent, selective, allosteric SHP2 inhibitor with IC50 of 36 nM, shows with impressive hERG selectivity (IC50>30 uM).
SHP389 inhibits p-ERK in KYSE-520 cells with IC50 of 36 nM, and shows antiproliferation effect with IC50 of 0.36 uM.
SHP389 demonstrated a moderate-high clearance ~83% hepatic extraction) which was under predicted in vitro by rat liver microsomes (Cl= 26.1 uL/min/mg, T1/2 = 53.2 min) assuming a hepatic blood flow of 55 mL/min/kg.
SHP389 also showed low oral bioavailability (~2 %F).

Physicochemical Properties

M.Wt 484.989
Formula C23H29ClN8O2
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

6-((3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl)-3-(3-chloro-2-(cyclopropylamino)pyridin-4-yl)-5-methyl-2,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one

References

1. Bagdanoff JT, et al. J Med Chem. 2019 Feb 8. doi: 10.1021/acs.jmedchem.8b01725.

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