SHP-099 hydrochloride is a potent, selective, allosteric and orally bioavailable protein tyrosine phosphatase SHP2 inhibitor with IC50 of 71 nM.
SHP-099 hydrochloride exhibits excellent phosphatase selectivity profiling over a panel of 21 human phosphatases (including SHP1) and a panel of 66 serine-threonine and tyrosine kinases.
SHP-099 hydrochloride inhibits p-ERK with an IC50 of ~0.25 uM in SHP2- dependent MDA-MB-468 and KYSE520 cells, suppresses RAS–ERK signalling to inhibit the proliferation of receptor-tyrosine-kinase-driven human cancer cells in vitro and is efficacious in mouse tumour xenograft models.
Physicochemical Properties
M.Wt
388.7225
Formula
C16H20Cl3N5
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
DMSO: 4.1 mg/mL; H2O: 7.69 mg/mL (Need ultrasonic and warming)
