1. MAPK/ERK Pathway
    Stem Cell/Wnt
  2. ERK
  3. AZD-0364

AZD-0364 

Cat. No.: HY-111483 Purity: 99.75%
Handling Instructions

AZD-0364 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.

AZD-0364 Chemical Structure

AZD-0364 Chemical Structure

CAS No. : 2097416-76-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 308 In-stock
Estimated Time of Arrival: December 31
5 mg USD 280 In-stock
Estimated Time of Arrival: December 31
10 mg USD 480 In-stock
Estimated Time of Arrival: December 31
25 mg USD 950 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1700 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Protocol

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  • References

Description

AZD-0364 is a potent and selective ERK2 inhibitor extracted from patent WO2017080979A1, compound example 18, has an IC50 of 0.6 nM.

IC50 & Target

IC50: 0.6 nM (ERK2)[1]

In Vitro

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].

In Vivo

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].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (202.22 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.21 mM); Clear solution

  • 2.

    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

  • 3.

    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

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

494.50

Formula

C₂₄H₂₄F₂N₈O₂

CAS No.

2097416-76-5

SMILES

O=C1C2=NC(C3=NC(NC4=CC=NN4C)=NC=C3C)=CN2C[[email protected]](COC)N1CC5=CC=C(F)C(F)=C5

Shipping

Room temperature in continental US; may vary elsewhere

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AZD-0364
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AZD-0364

Cat. No.: HY-111483