ChemicalBook--->CAS DataBase List--->1648863-90-4

1648863-90-4

1648863-90-4 Structure

1648863-90-4 Structure
IdentificationBack Directory
[Name]

G-5555
[CAS]

1648863-90-4
[Synonyms]

G-5555
G5555;G 5555
8-(((2r,5r)-5-Amino-1,3-dioxan-2-yl)methyl)-6-(2-chloro-4-(6-methylpyridin-2-yl)phenyl)-2-(met
8-[(trans-5-Amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(methylamino)-pyrido[2,3-d]pyrimidin-7(8H)-one
Pyrido[2,3-d]pyrimidin-7(8H)-one, 8-[(trans-5-amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(methylamino)-
[Molecular Formula]

C25H25ClN6O3
[MDL Number]

MFCD28506227
[MOL File]

1648863-90-4.mol
[Molecular Weight]

492.96
Chemical PropertiesBack Directory
[Boiling point ]

684.6±65.0 °C(Predicted)
[density ]

1.363±0.06 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMF: 25 mg/ml; DMSO: 25 mg/ml; DMSO:PBS(pH 7.2) (1:4): 0.20 mg/ml
[form ]

A crystalline solid
[pka]

6.86±0.40(Predicted)
[color ]

White to light yellow
Safety DataBack Directory
[Symbol(GHS) ]


GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319-H335
[Precautionary statements ]

P261-P305+P351+P338
Hazard InformationBack Directory
[Description]

G-5555 is an inhibitor of p21-activated kinase 1 (PAK1; Ki = 3.7 nM), a non-receptor serine/threonine kinase involved in tumorigenesis. It is selective for PAK1 over the majority of targets in a panel of 235 kinases but does inhibit PAK2, PAK3, KHS1, LCK, MST3, MST4, SIK2, and YSK1 by greater than 70% with IC50 values ranging from 9 to 52 nM. G-5555 inhibits phosphorylation of MEK, a downstream target of PAK1, in EBC1 cells (IC50 = 69 nM). G-5555 (10, 20, and 30 mg/kg) dose-dependently reduces phosphorylation of MEK in tumors from an H292 non-small cell lung cancer (NSCLC) mouse xenograft model. G-5555 inhibits hERG channels less than 50% at a concentration of 10 μM, indicating the potential for a low risk of QT interval prolongation and potentially fatal arrhythmias.
[Uses]

G 5555 is a high affinity group 1 p21-activated kinases (PAK) inhibitor.
[storage]

Store at -20°C
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