AZD0364
- Product Name
- AZD0364
- CAS No.
- 2097416-76-5
- Chemical Name
- AZD0364
- Synonyms
- CS-2696;AZD0364;ADZ0346;Tizaterkib;ERK2 inhibitor;AZD0364 (ATG-017);AZD-0364/Tizaterkib;AZD0364 (ATG-017) ,S8708;Tizaterkib, 10 mM in DMSO;AZD 0364;AZD0364;ERK2 INHIBITOR
- CBNumber
- CB93379847
- Molecular Formula
- C24H24F2N8O2
- Formula Weight
- 494.5
- MOL File
- 2097416-76-5.mol
AZD0364 Property
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 29827
- Product name
- AZD 0364
- Packaging
- 1mg
- Price
- $97
- Updated
- 2024/03/01
- Product number
- 29827
- Product name
- AZD 0364
- Packaging
- 10mg
- Price
- $672
- Updated
- 2024/03/01
- Product number
- 29827
- Product name
- AZD 0364
- Packaging
- 5mg
- Price
- $410
- Updated
- 2024/03/01
- Product number
- 6635EJ
- Product name
- (6R)-7-[(3,4-Difluorophenyl)methyl]-6-(methoxymethyl)-2-[5-methyl-2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]-5,6-dihydroimidazo[1,2-a]pyrazin-8-one
- Packaging
- 1mg
- Price
- $206
- Updated
- 2021/12/16
- Product number
- CS-0042190
- Product name
- AZD-0364
- Purity
- 99.75%
- Packaging
- 5mg
- Price
- $280
- Updated
- 2021/12/16
AZD0364 Chemical Properties,Usage,Production
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
Raw materials
Preparation Products
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