AZD-0364 (Synonyms: AZD0364) |
| Catalog No.GC19048 |
AZD-0364 (AZD0364) est un inhibiteur puissant et sélectif de ERK2 extrait du brevet WO2017080979A1, exemple composé 18, a une IC50 de 0,6 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2097416-76-5
Sample solution is provided at 25 µL, 10mM.
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AZD-0364 is a potent and selective ERK2 inhibitor extracted from patent WO2017080979A1, compound example 18, has an IC50 of 0.6 nM.
AZD-0364 is measured in the ERK2 mass spectrometry and A375 phospho-p90RSK assays with IC50s of 0.6 nM and 5.7 nM, respectively. AZD-0364 can inhibit the growth of a panel of cancer cell lines (A549, H2122, H2009, and Calu6 cell lines) with KRAS mutations as a monotherapy and this effect is synergistically enhanced by treatment with Selumetinib[1].
Tumor growth inhibition by AZD-0364 ethanesulfonic acid (Example 18a) in combination with MEK inhibitor Selumetinib is measured. Studies are performed in the A549 xenograft model. Selumetinib is dosed twice daily (BiD) 8 hours apart and AZD-0364 ethanesulfonic acid is dosed once daily (QD) 4 hours after the first Selumetinib dose. Both compounds are dosed continuously for 3 weeks. Both vehicles are dosed in the vehicle group. Both Selumetinib and AZD-0364 ethanesulfonic acid reduce tumor growth relative to vehicle only control. The combination of Selumetinib and AZD-0364 ethanesulfonic acid results in a reduction in tumor growth[1].
References:
[1]. WARD, Richard, Andrew, et al. DIHYDROIMIDAZOPYRAZINONE DERIVATIVES USEFUL IN THE TREATMENT OF CANCER. WO2017080979A1.
Cell experiment: | KRAS-mutant Non-Small Cell Lung Cancer (NSCLC) A549, H2122, H2009, and Calu6 cell lines are seeded in 384-well black, clear bottomed plates, cultured for 18-24 hours and treated with increasing concentrations of AZD-0364 (7.143 nM, 61 nM, 357 nM, 2.143 μM and 10 μM) and Selumetinib (0-10 μM) in a 6×6 dosing matrix. Cells are seeded at a concentration such that cells in untreated wells are approximately 80% confluent at the end of the assay. After 3 days of treatment, live cell number is determined using a Sytox Green endpoint[1]. |
Animal experiment: | Mice[1]A549 is a human non small cell lung cancer line carrying an oncogenic mutation in the KRAS gene (G12S). Female nude mice are implanted subcutaneously (s.c.) on the left flank, with 5×106 A549 cells (ATCC) per mouse.Tumor growth is monitored by twice weekly calliper measurement and volumes are calculated. Once tumors have reached a volume of ~200-300mm3 animals are randomised into groups of 7-11 and are treated with a continuous combination schedule of Selumetinib (ARRY-142886) 25 mg/kg BiD and AZD-0364 ethanesulfonic acid 25 mg/kg QD (four hours after first Selumetinib dose), both are dosed by peroral route. Tumor volumes are measured twice weekly after dosing commenced[1]. |
References: [1]. WARD, Richard, Andrew, et al. DIHYDROIMIDAZOPYRAZINONE DERIVATIVES USEFUL IN THE TREATMENT OF CANCER. WO2017080979A1. | |
| Cas No. | 2097416-76-5 | SDF | |
| Synonymes | AZD0364 | ||
| Canonical SMILES | O=C1C2=NC(C3=NC(NC4=CC=NN4C)=NC=C3C)=CN2C[C@H](COC)N1CC5=CC=C(F)C(F)=C5 | ||
| Formula | C24H24F2N8O2 | M.Wt | 494.5 |
| Solubility | DMSO : ≥ 100 mg/mL (202.22 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.0222 mL | 10.1112 mL | 20.2224 mL |
| 5 mM | 0.4044 mL | 2.0222 mL | 4.0445 mL |
| 10 mM | 0.2022 mL | 1.0111 mL | 2.0222 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)
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