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AZD1208

Name: AZD1208
Brand: Selleck Chemicals
SKU: S7104
Rating: 5 (31 reviews)

Catalog No.S7104

For research use only.

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.

CAS No. 1204144-28-4

Selleck's AZD1208 has been cited by 31 publications

Purity & Quality Control

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Pim Signaling Pathway Map

Biological Activity

Description

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

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 Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

MOLM16 cells	NIH5cZRRem:uaX\ldoF1cW:wIHHzd4F6		NX;YbYE{PzJiaB?=		NVva[o5OSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xOOTZiY3XscJMh[W[2ZYKgO\|IhcHK\|IHL5JGNmdGxiVHn0[ZIuSmy3ZTDhd5NigSxiR1m1NF0xNjB{IN88US=>	MnjnNlI4Ojd4NEC=

Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	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

AZD1208 suppresses the growth of MOLM-16 and KG-1a xenograft tumors in vivo in a dose proportional manner. ^[1]

Protocol (from reference)

References

[1] Erika Keeton, et al. 53rd ASH Annual Meeting (2011) Abstract nr 1540

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight	379.48
Formula	C₂₁H₂₁N₃O₂S
CAS No.	1204144-28-4
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	C1CC(CN(C1)C2=C(C=CC=C2C3=CC=CC=C3)C=C4C(=O)NC(=O)S4)N

Download AZD1208 SDF

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01489722	Terminated	Drug: AZD1208	Acute Myeloid Leukemia	AstraZeneca	February 2012	Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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.

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