Home JAK/STAT Pim inhibitor - Autophagy activator - Apoptosis related activator AZD1208 For research use only.

AZD1208

AZD1208 is a potent, and orally available Pim kinase inhibitor with IC50 of 0.4 nM, 5 nM, and 1.9 nM for Pim1, Pim2, and Pim3 in cell-free assays, respectively. AZD1208 induces autophagy, cell cycle arrest and apoptosis. Phase 1.

AZD1208 Chemical Structure

AZD1208 Chemical Structure

CAS: 1204144-28-4

Selleck's AZD1208 has been cited by 36 publications

Purity & Quality Control

Batch: Purity: 99.86%
99.86

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MOLM16 cells Proliferation assay 72 h Antiproliferative activity against human MOLM16 cells after 72 hrs by Cell Titer-Blue assay, GI50=0.02 μM 22727640
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Biological Activity

Description AZD1208 is a potent, and orally available Pim kinase inhibitor with IC50 of 0.4 nM, 5 nM, and 1.9 nM for Pim1, Pim2, and Pim3 in cell-free assays, respectively. AZD1208 induces autophagy, cell cycle arrest and apoptosis. Phase 1.
Features Orally bioavailable Pim kinase inhibitor that has been tested in Phase I clinical trials for treatment of advanced solid tumors and malignant lymphoma.
Targets
Pim1 [1]
(Cell-free assay)		 Pim3 [1]
(Cell-free assay)		 Pim2 [1]
(Cell-free assay)
0.4 nM 1.9 nM 5 nM
In vitro
In vitro

AZD1208 is an orally available, potent and highly selective Pim inhibitor that effectively inhibits all three isoforms. AZD1208 inhibits the growth of several AML cell lines and sensitivity correlates with the level of Pim-1 expression, STAT5 activation and presence of protein tyrosine kinase mutation. AZD1208 causes cell cycle arrest and apoptosis in MOLM-16 cells in culture. This is accompanied by a dose-dependent reduction in phosphorylation of BAD, 4EBP1 and p70S6K. In addition, AZD1208 leads to potent inhibition of colony growth of primary AML cells from bone marrow aspirates and downregulates phosphorylation of Pim targets. [1]
Cell Research Cell lines MDSCs
Concentrations 1 μM
Incubation Time 4 h
Method

Bone marrow derived MDSCs were separated into M-MDCSs and suppressive neutrophils by FACS, then plated in RPMI with 10% FBS in the presence of DMSO or AZD1208 for 4 hours on coverslips.
Experimental Result Images Methods Biomarkers Images PMID
Western blot Cleaved PARP / Myc / p-PRAS40 / PRAS40 / p-S6 / p-4EBP1 / 4EBP1 / p-BAD / BAD p-MKK4 / p-p38 / p-MK2 / p-AKT 27270648
Immunofluorescence p-Chk2 29879757
Growth inhibition assay Cell viability 30654529
In Vivo
In vivo

AZD1208 suppresses the growth of MOLM-16 and KG-1a xenograft tumors in vivo in a dose proportional manner. [1]
Animal Research Animal Models Female CB17 SCID mice
Dosages 10 & 30 mg/kg
Administration o.g.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01489722 Terminated Acute Myeloid Leukemia AstraZeneca February 2012 Phase 1

Chemical lnformation & Solubility

Molecular Weight 379.48 Formula

C21H21N3O2S
CAS No. 1204144-28-4 SDF Download AZD1208 SDF
Smiles C1CC(CN(C1)C2=C(C=CC=C2C3=CC=CC=C3)C=C4C(=O)NC(=O)S4)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 75 mg/mL ( (197.63 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.

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

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Frequently Asked Questions

Question 1:
What is your recommended solvent of S7104 for mouse in vivo studies by oral administration?

Answer:
1%CMC-Na is recommended and you will get a suspension. It is ok for oral administration.

Question 2:
I would like to ask which solvent I should use to dissolve AZD1208 for mouse study. Can AZD1208 be dissolved in 5% dextrose?

Answer:
AZ1208 can be dissolved in 5% dextrose at 10 mg/ml as a suspension. If 5% Tween 80 added, the suspension will be more homogeneously.

Pim Signaling Pathway Map

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