Chemical Structure : SHP2 inhibitor 14
CAS No.:
2055937-44-3
SHP2 inhibitor 14
Catalog No.: PC-36051Not For Human Use, Lab Use Only.
SHP2 inhibitor 14 is a novel potent, selective, allosteric, orally acitve SHP2 inhibitor with IC50 of 28 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
SHP2 inhibitor 14 is a novel potent, selective, allosteric, orally acitve SHP2 inhibitor with IC50 of 28 nM; inhibits p-ERK in KYSE-520 cells with IC50 of 93 nM, and shows antiproliferation effect with IC50 of 0.167 uM; demonstrates acceptable stability in mouse liver microsomes (Cl = 36.8, uL/min/mg, T1/2 = 60.2 min) and is sufficiently soluble (pH = 6.8 equilibrium solubility = 0.42 mM) to enable PK pharmacokinetic evaluation; modulate MAPK signaling in vivo in mice subcutaneously implanted with the KYSE520 carcinoma cell line.
Physicochemical Properties
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M.Wt
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463.363
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Formula
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C21H24Cl2N6O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20 °C 12 Months; 4°C 6 Months
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- In Solvent
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-80 °C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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6-((3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl)-3-(2,3-dichlorophenyl)-5-methyl-2,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
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References
1. Bagdanoff JT, et al. J Med Chem. 2019 Feb 8. doi: 10.1021/acs.jmedchem.8b01725.
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