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SHP-099 hydrochloride

Chemical Structure : SHP-099 hydrochloride

CAS No.: 1801747-11-4

SHP-099 hydrochloride (SHP099 hydrochloride)

Catalog No.: PC-42129Not For Human Use, Lab Use Only.

SHP-099 hydrochloride is a potent, selective, allosteric and orally bioavailable protein tyrosine phosphatase SHP2 inhibitor with IC50 of 71 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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)

Chemical Name/SMILES

2-Pyrazinamine, 6-(4-amino-4-methyl-1-piperidinyl)-3-(2,3-dichlorophenyl)-, hydrochloride (1:x)

References

1. Garcia Fortanet J, et al. J Med Chem. 2016 Sep 8;59(17):7773-82.

2. Chen YN, et al. Nature. 2016 Jul 7;535(7610):148-52.

3. Flemming A. Nat Rev Drug Discov. 2016 Jul 29;15(8):530-1.

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