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Chemical Structure : SHP389
CAS No.: 2235394-90-6
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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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).
| M.Wt | 484.989 | |
| Formula | C23H29ClN8O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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1. Bagdanoff JT, et al. J Med Chem. 2019 Feb 8. doi: 10.1021/acs.jmedchem.8b01725.
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