| Identification | Back 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 Properties | Back 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) |
| Hazard Information | Back 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]
| Target | Value | ERK2
() | 0.6 nM |
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