Chemical Structure : SHP-099 hydrochloride
CAS No.: 1801747-11-4
货号: 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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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.
分子量 | 388.7225 | |
分子式 | C16H20Cl3N5 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
DMSO: 4.1 mg/mL; H2O: 7.69 mg/mL (Need ultrasonic and warming) |
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Chemical Name/SMILES |
2-Pyrazinamine, 6-(4-amino-4-methyl-1-piperidinyl)-3-(2,3-dichlorophenyl)-, hydrochloride (1:x) |
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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