1. JAK/STAT Signaling
    Autophagy
  2. Pim
    Autophagy
  3. AZD1208

AZD1208 

Cat. No.: HY-15604 Purity: 99.67%
Handling Instructions

AZD1208 is a novel, orally bioavailable, highly selective PIM kinases inhibitor.

For research use only. We do not sell to patients.

AZD1208 Chemical Structure

AZD1208 Chemical Structure

CAS No. : 1204144-28-4

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10 mM * 1 mL in DMSO USD 79 In-stock
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50 mg USD 300 In-stock
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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of AZD1208:

Top Publications Citing Use of Products

    AZD1208 purchased from MCE. Usage Cited in: ENeuro. 2019 Aug 22;6(4). pii: ENEURO.0003-19.2019.

    PIM and PRK kinases function similarly in vitro. PRK-1 autophosphorylation was analysed in the absence (-) or presence (+) of 10 μM DHPCC-9, AZD-1208 and SGI-1776. The phosphorylated protein was visualized by immunoblotting with the phospho-RXXS*/T* antibody, which has several potential target sites in PRK-1.
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    Description

    AZD1208 is a novel, orally bioavailable, highly selective PIM kinases inhibitor.

    In Vitro

    AZD1208 shows good antiproliferative activity in a megakaryoblastic leukemia cell line, MOLM-16, with GI50 values less than 100 nM[1]. AZD1208 (10 μM) inhibits the growth of Ramos cells, and at 1 μM, strongly inhibits PIM kinases in all cell at 1 μM. AZD1208 induces apoptosis, and PIM2 knockdown is mainly associated with an alteration of the cell cycle[2]. The combination of AZD1208 and AZD2014 rapidly activates AMPKα, a negative regulator of translation machinery through mTORC1/2 signaling in AML cells; profoundly inhibits AKT and 4EBP1 activation; and suppresses polysome formation[3].

    Clinical Trial
    Molecular Weight

    379.48

    Formula

    C₂₁H₂₁N₃O₂S

    CAS No.

    1204144-28-4

    SMILES

    O=C(NC/1=O)SC1=C/C2=C(N3C[[email protected]](N)CCC3)C(C4=CC=CC=C4)=CC=C2

    Shipping

    Room temperature in continental US; may vary elsewhere

    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 : 28.5 mg/mL (75.10 mM; Need ultrasonic and warming)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6352 mL 13.1759 mL 26.3519 mL
    5 mM 0.5270 mL 2.6352 mL 5.2704 mL
    10 mM 0.2635 mL 1.3176 mL 2.6352 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [1]

    The activity of purified human PIM-1, PIM-2 and PIM-3 enzymes on substrate FL-Ahx-Bad (FITC-(AHX)RSRHSSYPAGT-COOH) is determined using a mobility shift assay on a Caliper LC3000 reader. The PIM-1 assay is performed in a 12 mL reaction containing 50 mM HEPES (pH 7.5), 1 mM DTT, 0.01% Tween 20, 50 mg/mL BSA, 10 mM MgCl2, 1.5 mM FL-Ahx-Bad peptide, 100 mM ATP, 2.5 nM PIM-1 and various amount of inhibitor. The reaction is quenched after 90 minute incubation at 25°C with 5 mL of stop mix consisting of 100 mM HEPES, 121 mM EDTA, 0.8% Coating Reagent 3 and 0.01% Tween 20. The ATP and enzyme concentrations for the PIM-2 assay are 5 mM and 2.5 nM, respectively, while 50 mM of ATP and 0.33 nM of enzyme is used for PIM-3 assays. For high [ATP] screenings, 5 mM ATP is used with 0.67 nM enzyme for both PIM-1 and PIM-2 or 0.11 nM PIM-3. Fluorescence of phosphorylated and unphosphorylated substrate is detected and a ratiometric value is calculated to determine percent turnover. IC50 values are determined from dose-response data using IDBS ActivityBase software.

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

    Cell Assay
    [1]

    MOLM-16 cells, purchased from DSMZ and cultured in RPMI containing 10% fetal bovine serum (FBS) and 1% L-glutamine, are plated at 20,000 cells per well in 96 well plates overnight. Cells are treated for 72 hours with compound or control vehicle (dimethyl sulfoxide) and cell viability is measured after the addition of Cell Titer-Blue for 4 hours at 37°C and reading of fluorescence on a Tecan Infinite® 200. The GI50 is determined by calculating growth at each dose relative to vehicle treated cells and cell viability at the time of treatment.

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

    References

    Purity: 99.67%

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    AZD1208
    Cat. No.:
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