AZ31

Catalog No.S8556

AZ31 Chemical Structure

Molecular Weight(MW): 420.50

AZ31 is a selective and novel ATM inhibitor with an IC50 of <0.0012 μM. It shows excellent selectivity over closely related enzymes (>500 fold selective over DNA-PK and PI3Kα and >1000 fold selective over mTOR, PI3Kβ and PI3Kγ).

Size Price Stock Quantity  
USD 147 In stock
USD 470 In stock
Bulk Discount
Bulk Inquiry

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Purity & Quality Control

Choose Selective ATM/ATR Inhibitors

Biological Activity

Description AZ31 is a selective and novel ATM inhibitor with an IC50 of <0.0012 μM. It shows excellent selectivity over closely related enzymes (>500 fold selective over DNA-PK and PI3Kα and >1000 fold selective over mTOR, PI3Kβ and PI3Kγ).
Targets
ATM [2]
()
In vitro

Antitumor effects of AZ31 + SN38 are cytostatic rather than cytotoxic[1].
In vivo

Pharmacokinetic investigation of AZ31 as a single agent and in combination with irinotecan revealed that plasma concentrations of AZ31 were highest 1-hour after administration followed by a stepwise decrease at 3, 6 and 16 hour in the combination sensitive CRC098[1].

Protocol

Kinase Assay:

[2]
+ Expand

ATM enzyme assay:

Compounds in 100% DMSO were added to assay plates by acoustic dispensing. ATM enzyme was added in a Hepes buffer (50 mM HEPES pH 7.4, 150 mM NaCl, 10 mM, MnCl2 1 mM, DTT, 5% v/v Glycerol, 0.05% v/v Tween 20) and allowed to preincubate with compound for 30 minutes prior to addition of substrate solution containing p53 and ATP. The enzyme reaction was stopped after 2 hours by the addition of detection reagent (33 mM HEPES pH 7.4, 20 mM EDTA, 0.1 M KF, 0.1 mg/mL BSA, 13 nM D2 Anti-GST antibody (Cisbio) and 0.5 nM Eu3+ Anti-p53phosphoS15 antibody) and incubated overnight before reading on a Pherastar Instrument with a standard HTRF filter block method. The final concentrations of DMSO, ATP and p53 in the assay were 1%, 5 µM, and 50 nM respectively. IC50 values (concentrations of test compound that inhibited 50% of enzyme activity) were determined using a four parameter fit method (smart fitting model) in the data analysis software.
Cell Research:

[1]
+ Expand
  • Cell lines: CRC (metastatic colorectal cancer) cell lines: HCT15, HCT116, RKO, CaCo2, LS123 and LOVO
  • Concentrations: 1.25, 2.5 or 5 μmol/L
  • Incubation Time: 72 hours
  • Method:

    Six CRC cell lines were treated with AZ31 (dose 1.25, 2.5 or 5 μmol/L), SN38 (0.3125 -20 nM) or AZ31 + SN38 and proliferation was determined by an SRB assay.


    (Only for Reference)
Animal Research:

[1]
+ Expand
  • Animal Models: CRC PDX models (Four-to-six week-old female athymic nude mice with implanted patient-derived colorectal adenocarcinoma tumor)
  • Formulation: 10% v/v DMSO + 90% v/v Captisol at 30% w/v
  • Dosages: 100 mg/kg-daily × 3
  • Administration: by oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 53 mg/mL (126.04 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 420.50
Formula

C24H28N4O3
CAS No. 2088113-98-6
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field
selleck catalog

ATM/ATR Signaling Pathway Map

Related ATM/ATR Products0

  • AZD6738 New

    AZD6738 is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.

  • CHIR-99021 (CT99021) New

    CHIR-99021 (CT99021) is a GSK-3α and GSK-3β inhibitor with IC50 of 10 nM and 6.7 nM, respectively. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) and shows a 350-fold selectivity toward GSK-3β compared to CDKs.

  • Dorsomorphin (Compound C) New

    Dorsomorphin is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type I BMP receptor activity.

  • KU-55933 (ATM Kinase Inhibitor)

    KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor with IC50/Ki of 12.9 nM/2.2 nM in cell-free assays, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.

  • VE-821

    VE-821 is a potent and selective ATP competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM in cell-free assays, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ.

  • KU-60019

    KU-60019 is an improved analogue of KU-55933, with IC50 of 6.3 nM for ATM in cell-free assays, 270- and 1600-fold more selective for ATM than DNA-PK and ATR,and is a highly effective radiosensitizer.

    Features:Improved analog of KU-55933, and is more effective at blocking ATM-mediated DDR events.

  • Berzosertib (VE-822|VX970|M6620)

    VE-822 is an ATR inhibitor with IC50 of 19 nM in HT29 cells.

    Features:VE-822 is a highly selective and potent derivative of the ATR inhibitor VE-821.

  • Chloroquine diphosphate

    Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator.

  • AZ20

    AZ20 is a novel potent and selective inhibitor of ATR kinase with IC50 of 5 nM in a cell-free assay, 8-fold selectivity over mTOR.

    Features:AZ20 is the first reported inhibitor of ATR protein kinase demonstrating tumor growth inhibition in vivo.

  • CP-466722

    CP-466722 is a potent and reversible ATM inhibitor, does not affect ATR and inhibits PI3K or PIKK family members in cells.

Tags: buy AZ31 | AZ31 supplier | purchase AZ31 | AZ31 cost | AZ31 manufacturer | order AZ31 | AZ31 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID