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AZD1208 Pim inhibitor

Name: AZD1208
Brand: Selleck Chemicals
SKU: S7104
Availability: InStock
Rating: 5 (41 reviews)

Cat.No.S7104

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. This compound induces autophagy, cell cycle arrest and apoptosis. Phase 1.

Chemical Structure

Molecular Weight: 379.48

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.86%

99.86

Related Targets	EGFR JAK STAT
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Cell Culture, Treatment & Working Concentration

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
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	379.48	Formula	C₂₁H₂₁N₃O₂S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1204144-28-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1CC(CN(C1)C2=C(C=CC=C2C3=CC=CC=C3)C=C4C(=O)NC(=O)S4)N

Solubility

In vitro
Batch:

DMSO : 75 mg/mL (197.63 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.800mg/ml (10.01mM)	Taking the 1 mL working solution as an example, add 50 μL of clarified DMSO stock solution of 76 mg/ml to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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.

Mechanism of Action

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/IC₅₀/Ki	Pim1 ^[1] (Cell-free assay) 0.4 nM Pim3 ^[1] (Cell-free assay) 1.9 nM Pim2 ^[1] (Cell-free assay) 5 nM
In vitro	AZD1208 is an orally available, potent and highly selective Pim inhibitor that effectively inhibits all three isoforms. This compound 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. It 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, this chemical leads to potent inhibition of colony growth of primary AML cells from bone marrow aspirates and downregulates phosphorylation of Pim targets. ^[1]
In vivo	AZD1208 suppresses the growth of MOLM-16 and KG-1a xenograft tumors in vivo in a dose proportional manner. ^[1]
References	[1] https://ash.confex.com/ash/2011/webprogram/Paper41793.html [2] https://pubmed.ncbi.nlm.nih.gov/34038722/ [3] https://pubmed.ncbi.nlm.nih.gov/24363397/

Applications

Methods	Biomarkers	PMID
Western blot	p-MKK4 / p-p38 / p-MK2 / p-AKT Cleaved PARP / Myc / p-PRAS40 / PRAS40 / p-S6 / p-4EBP1 / 4EBP1 / p-BAD / BAD	27270648
Immunofluorescence	p-Chk2	29879757
Growth inhibition assay	Cell viability	30654529

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

Tech Support

Handling Instructions

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

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Frequently Asked Questions

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

Answer:
It is recommended to use 1% CMC-Na, which will result in a suspension. This compound is suitable for oral administration.

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

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

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