Tizaterkib
Based on 3 publication(s) in Google Scholar
Tizaterkib (AZD0364) is a potent and selective ERK2 inhibitor extracted from patent WO2017080979A1, compound example 18, has an IC50 of 0.6 nM.
For research use only. We do not sell to patients.
- Purity: 99.10%
- CAS No.: 2097416-76-5
- Formula: C24H24F2N8O2
- Molecular Weight:494.50
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Tizaterkib
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Biological Activity
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ERK2 0.6 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | GI50 |
0.06 μM
Compound: 15; AZD0364
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Antiproliferative activity at human A375 cells expressing BRAF V600E mutant assessed as growth inhibition
Antiproliferative activity at human A375 cells expressing BRAF V600E mutant assessed as growth inhibition
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[PMID: 31710489] |
| Calu-6 | GI50 |
0.2 μM
Compound: 15; AZD0364
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Antiproliferative activity against human Calu6 cells expressing KRAS Q61K mutant assessed as growth inhibition
Antiproliferative activity against human Calu6 cells expressing KRAS Q61K mutant assessed as growth inhibition
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[PMID: 31710489] |
| Sf21 | IC50 |
1 μM
Compound: 15; AZD0364
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Inhibition of human full length C-terminal His6-tagged Cdk2/human full length N-terminal GST-tagged Cyclin E expressed in baculovirus infected Sf21 insect cells after 1 hr by electromobility shift assay
Inhibition of human full length C-terminal His6-tagged Cdk2/human full length N-terminal GST-tagged Cyclin E expressed in baculovirus infected Sf21 insect cells after 1 hr by electromobility shift assay
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[PMID: 31710489] |
Tizaterkib is measured in the ERK2 mass spectrometry and A375 phospho-p90RSK assays with IC50s of 0.6 nM and 5.7 nM, respectively. Tizaterkib 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2097416-76-5
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Appearance Solid
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Molecular Weight 494.50
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Formula C24H24F2N8O2
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Color White to off-white
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SMILES
O=C1C2=NC(C3=NC(NC4=CC=NN4C)=NC=C3C)=CN2C[C@H](COC)N1CC5=CC=C(F)C(F)=C5
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Synonyms
AZD0364
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Int J Mol Sci
ERK1/2 Inhibition via the Oral Administration of Tizaterkib Alleviates Noise-Induced Hearing Loss While Tempering down the Immune Response. [Abstract]2024 Jun 7;25(12):6305. PMID: 38928015 -
Vet Microbiol
Highly pathogenic porcine reproductive and respiratory syndrome virus (HP-PRRSV) induces IL-6 production through TAK-1/JNK/AP-1 and TAK-1/NF-κB signaling pathways. [Abstract]2021 May:256:109061. PMID: 33836390 -
bioRxiv
ERK1/2 Inhibition Alleviates Noise-Induced Hearing Loss While Tempering Down the Immune Response. [Abstract]2023 Oct 20:2023.10.18.563007. PMID: 37905140
Solvent & Solubility
DMSO : ≥ 100 mg/mL (202.22 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.21 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.21 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0222 mL | 10.1112 mL | 20.2224 mL | 50.5561 mL |
| 5 mM | 0.4044 mL | 2.0222 mL | 4.0445 mL | 10.1112 mL | |
| 10 mM | 0.2022 mL | 1.0111 mL | 2.0222 mL | 5.0556 mL | |
| 15 mM | 0.1348 mL | 0.6741 mL | 1.3482 mL | 3.3704 mL | |
| 20 mM | 0.1011 mL | 0.5056 mL | 1.0111 mL | 2.5278 mL | |
| 25 mM | 0.0809 mL | 0.4044 mL | 0.8089 mL | 2.0222 mL | |
| 30 mM | 0.0674 mL | 0.3370 mL | 0.6741 mL | 1.6852 mL | |
| 40 mM | 0.0506 mL | 0.2528 mL | 0.5056 mL | 1.2639 mL | |
| 50 mM | 0.0404 mL | 0.2022 mL | 0.4044 mL | 1.0111 mL | |
| 60 mM | 0.0337 mL | 0.1685 mL | 0.3370 mL | 0.8426 mL | |
| 80 mM | 0.0253 mL | 0.1264 mL | 0.2528 mL | 0.6320 mL | |
| 100 mM | 0.0202 mL | 0.1011 mL | 0.2022 mL | 0.5056 mL |
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