ChemicalBook--->CAS DataBase List--->2097416-76-5

2097416-76-5

2097416-76-5 Structure

2097416-76-5 Structure
IdentificationBack Directory
[Name]

AZD0364
[CAS]

2097416-76-5
[Synonyms]

AZD0364
CS-2696
ADZ0346
ERK2 inhibitor
AZD 0364;AZD0364;ERK2 INHIBITOR
Imidazo[1,2-a]pyrazin-8(5H)-one, 7-[(3,4-difluorophenyl)methyl]-6,7-dihydro-6-(methoxymethyl)-2-[5-methyl-2-[(1-methyl-1H-pyrazol-5-yl)amino]-4-pyrimidinyl]-, (6R)-
[Molecular Formula]

C24H24F2N8O2
[MDL Number]

MFCD31631580
[MOL File]

2097416-76-5.mol
[Molecular Weight]

494.5
Chemical PropertiesBack Directory
[Boiling point ]

716.0±70.0 °C(Predicted)
[density ]

1.45±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMSO:41.67(Max Conc. mg/mL);84.27(Max Conc. mM)
DMF:25.0(Max Conc. mg/mL);50.56(Max Conc. mM)
DMF:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);1.01(Max Conc. mM)
Ethanol:54.5(Max Conc. mg/mL);110.21(Max Conc. mM)
[form ]

A crystalline solid
[pka]

2?+-.0.10(Predicted)
[color ]

White to off-white
Safety DataBack Directory
[Symbol(GHS) ]

Exclamation Mark (GHS07)
GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319-H335
[Precautionary statements ]

P261-P305+P351+P338
Spectrum DetailBack Directory
[Spectrum Detail]

AZD0364(2097416-76-5)1HNMR
Hazard InformationBack Directory
[Biological Activity]

AZD0364 (ATG-017) is an ERK1/2 inhibitor with IC50 of 0.6 nM for ERK2.
[in vitro]

AZD0364 has high cellular activity against direct downstream substrates of the MAPK signaling pathway (as in BRAF.

[in vivo]

AZD0364 has good oral pharmacokinetics in various species. In a xenograft model, AZD0364 inhibited phosphorylated p90RSK1 in a concentration-dependent manner in tumors. AZD0634 induces tumor regression in a KRAS-mutated NSCLC Calu 6 xenograft model, in which AZD0634 can be safely and effectively administered in combination with selumetinib.

[target]

TargetValue
ERK2
()
0.6 nM
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