- Tizaterkib
-
- $96.00
-
2026-07-27
- CAS:2097416-76-5
- Purity: 99.63%
- Supply Ability: 10g
- Tizaterkib
-
- $96.00
-
2026-07-27
- CAS:2097416-76-5
- Purity: 99.63%
- Supply Ability: 10g
|
| | 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) | | color | White to off-white | | InChIKey | HVIGNZUDBVLTLU-MRXNPFEDSA-N | | SMILES | C12=NC(C3C(C)=CN=C(NC4N(C)N=CC=4)N=3)=CN1C[C@H](COC)N(CC1=CC=C(F)C(F)=C1)C2=O |
| | AZD0364 Usage And Synthesis |
| Uses | Tizaterkib (AZD0364) is a potent and selective ERK2 inhibitor extracted from patent WO2017080979A1, compound example 18, has an IC50 of 0.6 nM. | | 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 |
| | IC 50 | ERK2: 0.6 nM (IC50) | | References | [1] WARD, Richard, Andrew, et al. DIHYDROIMIDAZOPYRAZINONE DERIVATIVES USEFUL IN THE TREATMENT OF CANCER. WO2017080979A1. |
| | AZD0364 Preparation Products And Raw materials |
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