1. JAK/STAT Signaling
  2. Pim

AZD1208 hydrochloride 

Cat. No.: HY-15604A
Handling Instructions

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

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

AZD1208 hydrochloride Chemical Structure

AZD1208 hydrochloride Chemical Structure

CAS No. : 1621866-96-3

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10 mg USD 102 Get quote
50 mg USD 300 Get quote
100 mg USD 540 Get quote

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target

PIM[1]

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].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : 83.3 mg/mL (200.27 mM; Need ultrasonic and warming)

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
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

The activity of purified human PIM-1, PIM-2 and PIM-3 enzymes on substrate FL-Ahx-Bad is determined using a mobility shift assay on a 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 software[1].

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

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
Molecular Weight

415.94

Formula

C₂₁H₂₂ClN₃O₂S

CAS No.

1621866-96-3

SMILES

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

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
AZD1208 hydrochloride
Cat. No.:
HY-15604A
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AZD1208 hydrochloride

Cat. No.: HY-15604A