AZD1208 hydrochloride

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Data Sheet Handling Instructions

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

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

AZD1208 hydrochloride Chemical Structure

CAS No. : 1621866-96-3

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Other In-stock Forms of AZD1208 hydrochloride:

AZD1208

Other Forms of AZD1208 hydrochloride:

AZD1208 In-stock

15 Publications Citing Use of MCE AZD1208 hydrochloride

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•Related Small Molecules:

•Related Proteins:

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PIM1 PIM2 PIM3

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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

IC₅₀ & Target

PIM2

In Vitro

AZD1208 hydrochloride shows good antiproliferative activity in a megakaryoblastic leukemia cell line, MOLM-16, with GI₅₀ values less than 100 nM^[1]. AZD1208 hydrochloride (10 μM) inhibits the growth of Ramos cells, and at 1 μM, strongly inhibits PIM kinases in all cells at 1 μM. AZD1208 hydrochloride induces apoptosis, and PIM2 knockdown is mainly associated with an alteration of the cell cycle^[2]. The combination of AZD1208 hydrochloride 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.

Clinical Trial

Molecular Weight

415.94

Formula

C₂₁H₂₂ClN₃O₂S

CAS No.

1621866-96-3

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

In Vitro:

DMSO : 83.3 mg/mL (200.27 mM; Need ultrasonic and warming; 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	2.4042 mL	12.0210 mL	24.0419 mL
5 mM	0.4808 mL	2.4042 mL	4.8084 mL
10 mM	0.2404 mL	1.2021 mL	2.4042 mL

View the Complete Stock Solution Preparation Table

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

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 (including AZD1208 hydrochloride) 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^[1].

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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4042 mL	12.0210 mL	24.0419 mL	60.1048 mL
	5 mM	0.4808 mL	2.4042 mL	4.8084 mL	12.0210 mL
	10 mM	0.2404 mL	1.2021 mL	2.4042 mL	6.0105 mL
	15 mM	0.1603 mL	0.8014 mL	1.6028 mL	4.0070 mL
	20 mM	0.1202 mL	0.6010 mL	1.2021 mL	3.0052 mL
	25 mM	0.0962 mL	0.4808 mL	0.9617 mL	2.4042 mL
	30 mM	0.0801 mL	0.4007 mL	0.8014 mL	2.0035 mL
	40 mM	0.0601 mL	0.3005 mL	0.6010 mL	1.5026 mL
	50 mM	0.0481 mL	0.2404 mL	0.4808 mL	1.2021 mL
	60 mM	0.0401 mL	0.2003 mL	0.4007 mL	1.0017 mL
	80 mM	0.0301 mL	0.1503 mL	0.3005 mL	0.7513 mL
	100 mM	0.0240 mL	0.1202 mL	0.2404 mL	0.6010 mL