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AZD1208

Catalog No. T2300 CAS 1204144-28-4

AZD1208 is a novel, orally bioavailable, highly selective PIM kinase inhibitor with single nanomolar potency against all three PIM kinases.

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AZD1208, CAS 1204144-28-4

Pack Size	Availability	Price/USD
2 mg	In stock	$ 32.00
5 mg	In stock	$ 47.00
10 mg	In stock	$ 68.00
25 mg	In stock	$ 121.00
50 mg	In stock	$ 225.00
100 mg	In stock	$ 397.00
200 mg	In stock	$ 522.00
500 mg	In stock	$ 833.00
1 mL * 10 mM (in DMSO)	In stock	$ 52.00

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Purity: 98.87%

Purity: 97.24%

Biological Description

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Description	AZD1208 is a novel, orally bioavailable, highly selective PIM kinase inhibitor with single nanomolar potency against all three PIM kinases.
Targets&IC50	Pim1:0.4 nM, Pim3:1.9 nM, Pim2:5 nM
In vitro	AZD1208 dose-dependently inhibits the growth of MOLM-16 and KG-1a xenograft tumors in vivo.
In vivo	AZD1208 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.
Kinase Assay	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.
Cell Research	AZD1208 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.

Molecular Weight	379.48
Formula	C21H21N3O2S
CAS No.	1204144-28-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 7.6 mg/mL (20 mM), Heating is recommended.

References and Literature

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

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Inhibitor Library Kinase Inhibitor Library Anti-Cancer Drug Library Anti-Prostate Cancer Compound Library Autophagy Compound Library Epigenetics Compound Library JAK-STAT Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

AZD1208 1204144-28-4 Apoptosis Autophagy Chromatin/Epigenetic JAK/STAT signaling Pim inhibit AZD-1208 Pim kinases Inhibitor AZD 1208 inhibitor

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