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> AZD1208 [1204144-28-4]

AZD1208 [1204144-28-4]

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Cat# HY-15604-5mg

Size : 5mg

Brand : MedChemExpress


AZD1208 is an orally bioavailable, highly selective PIM kinases inhibitor.

For research use only. We do not sell to patients.

AZD1208 Chemical Structure

AZD1208 Chemical Structure

CAS No. : 1204144-28-4

This product is a controlled substance and not for sale in your territory.

Based on 14 publication(s) in Google Scholar

Other Forms of AZD1208:

  • AZD1208 hydrochloride Get quote

View All Pim Isoform Specific Products:

View All Isoforms
PIM1 PIM2 PIM3
Description

AZD1208 is an orally bioavailable, highly selective PIM kinases inhibitor[1].

IC50 & Target

PIM2

 

In Vitro

AZD1208 shows good antiproliferative activity in a megakaryoblastic leukemia cell line, MOLM-16, with GI50 values less than 100 nM[1].
AZD1208 (10 μM) inhibits the growth of Ramos cells, and at 1 μM, strongly inhibits PIM kinases in all cell at 1 μM. AZD1208 induces apoptosis, and PIM2 knockdown is mainly associated with an alteration of the cell cycle[2].
The combination of AZD1208 and AZD2014 rapidly activates AMPKα, a negative regulator of translation machinery through mTORC1/2 signaling in AML cells; profoundly inhibits AKT and 4EBP1 activation; and suppresses polysome formation[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AZD1208 Related Antibodies
Clinical Trial
Molecular Weight

379.48

Formula

C21H21N3O2S
CAS No.

1204144-28-4
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC/1=O)SC1=C/C2=C(N3C[C@H](N)CCC3)C(C4=CC=CC=C4)=CC=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (131.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6352 mL 13.1759 mL 26.3519 mL
5 mM 0.5270 mL 2.6352 mL 5.2704 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (13.18 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 5 mg/mL (13.18 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.71%

COA (253 KB) LCMS (264 KB)

Handling Instructions (2659 KB)
References

  • [1]. Dakin LA, et al. Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4599-604.  [Content Brief]

    [2]. Kreuz S, et al. Loss of PIM2 enhances the anti-proliferative effect of the pan-PIM kinase inhibitor AZD1208 in non-Hodgkin lymphomas. Mol Cancer. 2015 Dec 8;14:205.  [Content Brief]

    [3]. Harada M, et al. The novel combination of dual mTOR inhibitor AZD2014 and pan-PIM inhibitor AZD1208 inhibits growth in acute myeloid leukemia via HSF pathway suppression. Oncotarget. 2015 Nov 10;6(35):37930-47.  [Content Brief]

Cell Assay
[1]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

  • [1]. Dakin LA, et al. Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4599-604.  [Content Brief]

    [2]. Kreuz S, et al. Loss of PIM2 enhances the anti-proliferative effect of the pan-PIM kinase inhibitor AZD1208 in non-Hodgkin lymphomas. Mol Cancer. 2015 Dec 8;14:205.  [Content Brief]

    [3]. Harada M, et al. The novel combination of dual mTOR inhibitor AZD2014 and pan-PIM inhibitor AZD1208 inhibits growth in acute myeloid leukemia via HSF pathway suppression. Oncotarget. 2015 Nov 10;6(35):37930-47.  [Content Brief]

  • [1]. Dakin LA, et al. Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4599-604.

    [2]. Kreuz S, et al. Loss of PIM2 enhances the anti-proliferative effect of the pan-PIM kinase inhibitor AZD1208 in non-Hodgkin lymphomas. Mol Cancer. 2015 Dec 8;14:205.

    [3]. Harada M, et al. The novel combination of dual mTOR inhibitor AZD2014 and pan-PIM inhibitor AZD1208 inhibits growth in acute myeloid leukemia via HSF pathway suppression. Oncotarget. 2015 Nov 10;6(35):37930-47.

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6352 mL 13.1759 mL 26.3518 mL 65.8796 mL
5 mM 0.5270 mL 2.6352 mL 5.2704 mL 13.1759 mL
10 mM 0.2635 mL 1.3176 mL 2.6352 mL 6.5880 mL
15 mM 0.1757 mL 0.8784 mL 1.7568 mL 4.3920 mL
20 mM 0.1318 mL 0.6588 mL 1.3176 mL 3.2940 mL
25 mM 0.1054 mL 0.5270 mL 1.0541 mL 2.6352 mL
30 mM 0.0878 mL 0.4392 mL 0.8784 mL 2.1960 mL
40 mM 0.0659 mL 0.3294 mL 0.6588 mL 1.6470 mL
50 mM 0.0527 mL 0.2635 mL 0.5270 mL 1.3176 mL
60 mM 0.0439 mL 0.2196 mL 0.4392 mL 1.0980 mL
80 mM 0.0329 mL 0.1647 mL 0.3294 mL 0.8235 mL
100 mM 0.0264 mL 0.1318 mL 0.2635 mL 0.6588 mL
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AZD1208 Related Classifications

  • JAK/STAT Signaling Autophagy Apoptosis
  • Pim Autophagy Apoptosis
Help & FAQs

Keywords:

AZD12081204144-28-4AZD 1208AZD-1208PimAutophagyApoptosisPim kinasesInhibitorinhibitorinhibit

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