|
|
| | AZD0364 Basic information |
| Product Name: | AZD0364 | | Synonyms: | AZD0364;CS-2696;AZD 0364;AZD0364;ERK2 INHIBITOR;ERK2 inhibitor;ADZ0346;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)-;Tizaterkib;AZD-0364/Tizaterkib | | CAS: | 2097416-76-5 | | MF: | C24H24F2N8O2 | | MW: | 494.5 | | EINECS: | | | Product Categories: | API | | Mol File: | 2097416-76-5.mol |  |
| | AZD0364 Chemical Properties |
| 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) |
| | AZD0364 Usage And Synthesis |
| 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 |
|
| | AZD0364 Preparation Products And Raw materials |
|