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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Protein tyrosine kinase /JAK / STAT>Pim inhibitors>AZD1208
AZD1208
  • AZD1208

AZD1208 NEW

Price $32 $47 $68
Package 2mg 5mg 10mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: AZD1208 CAS No.: 1204144-28-4
Purity: 98.87% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameAZD1208
DescriptionAZD1208 is a novel, orally bioavailable, highly selective PIM kinase inhibitor with single nanomolar potency against all three PIM kinases.
Cell ResearchAZD1208 is dissolved in DMSO. 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.
Kinase AssayThe 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.
In vitroAZD1208 dose-dependently inhibits the growth of MOLM-16 and KG-1a xenograft tumors in vivo.
In vivoAZD1208 induces cell cycle arrest and apoptosis in cultured MOLM-16 cells, accompanied by a dose-dependent decrease in the phosphorylation of BAD, 4EBP1, and p70S6K. Additionally, AZD1208 effectively inhibits colony growth of primary AML cells derived from bone marrow aspirates and downregulates phosphorylation of Pim targets.
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationDMSO : 7.6 mg/mL (20 mM), Heating is recommended.
KeywordsPim | inhibit | Autophagy | Apoptosis | AZD-1208 | Pim kinases | Inhibitor | AZD 1208 | AZD1208
Inhibitors RelatedStavudine | 5-Fluorouracil | Sodium 4-phenylbutyrate | L-Ascorbic acid | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Tributyrin | Curcumin | Paeonol | Naringin | Gefitinib
Related Compound LibrariesApoptosis Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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