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AZD1208 [1204144-28-4]

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Referencia NB-64-12257-10mg

embalaje : 10mg

Marca : Neo Biotech

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AZD1208

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Synonyms:

Catalog No. T2300 Copy Product Info

Purity: 99.83%

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

Cas No. 1204144-28-4

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.83%

Color:Yellow

Product Information

Bioactivity

Description	AZD1208 is a novel, orally bioavailable, highly selective PIM kinase inhibitor with single nanomolar potency against all three PIM kinases.
Targets & IC50	Pim3:1.9 nM, Pim2:5 nM, Pim1:0.4 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.

Chemical Properties

Molecular Weight	379.48
Formula	C₂₁H₂₁N₃O₂S
Cas No.	1204144-28-4
Smiles	NC1CCCN(C1)c1c(\C=C2/SC(=O)NC2=O)cccc1-c1ccccc1
Relative Density.	1.307 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Keep away from moisture,Store under nitrogen,Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 50 mg/mL (131.76 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.64 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6352 mL	13.1759 mL	26.3518 mL	131.7592 mL
5 mM	0.5270 mL	2.6352 mL	5.2704 mL	26.3518 mL
10 mM	0.2635 mL	1.3176 mL	2.6352 mL	13.1759 mL
20 mM	0.1318 mL	0.6588 mL	1.3176 mL	6.5880 mL
50 mM	0.0527 mL	0.2635 mL	0.5270 mL	2.6352 mL
100 mM	0.0264 mL	0.1318 mL	0.2635 mL	1.3176 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

Pim3Pim2Pim1Pim kinasesPimInhibitorinhibitAZD-1208AZD1208AZD 1208AutophagyApoptosis

Related Tags: AZD1208 chemical structure | AZD1208 in vivo | AZD1208 in vitro | AZD1208 formula | AZD1208 molecular weight