AZ960

Cat. No.: HY-10411 Purity: 97.15%: FAQs
Data Sheet SDS COA Handling Instructions

AZ960 is a potent and specific inhibitor of the JAK2 kinase with a K_i of 0.45 nM.

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

AZ960 Chemical Structure

CAS No. : 905586-69-8

Size	Price	Stock	Quantity
Solution
10 mM * 1 mL in DMSO	USD 129	In-stock	Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL ready for reconstitution	USD 129	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 88	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 165	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 275	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 825	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1265	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

AZ960 is a potent and specific inhibitor of the JAK2 kinase with a K_i of 0.45 nM.

IC₅₀ & Target^[4]

JAK2

0.45 nM (Ki)

JAK2

<3 nM (IC₅₀)

JAK3

9 nM (IC₅₀)

In Vitro

AZ960 inhibits Jak2 kinase with a K_i of 0.45 nM. Z960 possesses much less potent activity against Jak1, 3, and TYK2. AZ960 is active against other kinases, including TrkA, Aurora-A, and FAK, with IC₅₀ of around 0.1 μM. AZ960 effectively induces growth arrest and apoptosis of human T-cell lymphotropic virus type 1, HTLV-1–infected T cells (MT-1 and MT-2) in parallel with downregulation of the phosphorylated forms of Jak2 and Bcl-2 family proteins including Bcl-2 and Mcl-1^[2]. AZ960 potently inhibits the clonogenic growth and induces apoptosis of freshly isolated acute myelogenous leukemia cells from patients in association with cleavage of caspase 3 and down regulation of anti-apoptotic Bcl-xL proteins^[1]. AZ960 has a K_i of 1.25 μM for T. brucei extracellular signal-regulated kinase 8 (TbERK8). It inhibits TbERK8 with an IC₅₀ of 120 nM^[3].

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

Molecular Weight

354.36

Appearance

Solid

Formula

C₁₈H₁₆F₂N₆

CAS No.

905586-69-8

SMILES

N#CC1=CC(F)=C(NC2=NNC(C)=C2)N=C1N[[email protected]](C3=CC=C(F)C=C3)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 30 mg/mL (84.66 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.8220 mL	14.1099 mL	28.2199 mL
5 mM	0.5644 mL	2.8220 mL	5.6440 mL
10 mM	0.2822 mL	1.4110 mL	2.8220 mL

*Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (7.05 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.05 mM); Clear solution

*All of the co-solvents are available by MCE.

Purity & Documentation

Purity: 97.15%

Select Batch:

Data Sheet (275 KB) SDS (251 KB)

COA (246 KB) RP-HPLC (243 KB)

Handling Instructions (2659 KB)

References

[1]. Ikezoe T, et al. Expression of p-JAK2 predicts clinical outcome and is a potential molecular target of acute myelogenous leukemia. Int J Cancer. 2011 Nov 15;129(10):2512-21. [Content Brief]

[2]. Gozgit JM, et al. Effects of the JAK2 inhibitor, AZ960, on Pim/BAD/BCL-xL survival signaling in the human JAK2 V617F cell line SET-2. J Biol Chem. 2008 Nov 21;283(47):32334-43. [Content Brief]

[3]. Yang J, et al. AZ960, a novel Jak2 inhibitor, induces growth arrest and apoptosis in adult T-cell leukemia cells. Mol Cancer Ther. 2010 Dec;9(12):3386-95. [Content Brief]

[4]. Valenciano AL, et al. Discovery and antiparasitic activity of AZ960 as a Trypanosoma brucei ERK8 inhibitor. Bioorg Med Chem. 2016 Oct 1;24(19):4647-51. [Content Brief]

Cell Assay
^[2]

AZ960 is dissolved in 100% DMSO to a 0.01 M. HTLV-1–infected T cells and MOLT-4 cells are cultured with various concentrations of AZ960 (0.03-1 μM) for 2 days in 96-well plates. Peripheral blood lymphocytes are activated by phytohemagglutinin (PHA; 5 ng/mL) for 1 hour, then cultured with various concentrations of AZ960 (0.03–1 μM) for 2 days in 96-well plates. After culture, cell number and viability are evaluated by measuring the mitochondrial-dependent conversion of the MTT to a colored formazan product^[2].

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

References

[1]. Ikezoe T, et al. Expression of p-JAK2 predicts clinical outcome and is a potential molecular target of acute myelogenous leukemia. Int J Cancer. 2011 Nov 15;129(10):2512-21. [Content Brief]

[2]. Gozgit JM, et al. Effects of the JAK2 inhibitor, AZ960, on Pim/BAD/BCL-xL survival signaling in the human JAK2 V617F cell line SET-2. J Biol Chem. 2008 Nov 21;283(47):32334-43. [Content Brief]

[3]. Yang J, et al. AZ960, a novel Jak2 inhibitor, induces growth arrest and apoptosis in adult T-cell leukemia cells. Mol Cancer Ther. 2010 Dec;9(12):3386-95. [Content Brief]

[4]. Valenciano AL, et al. Discovery and antiparasitic activity of AZ960 as a Trypanosoma brucei ERK8 inhibitor. Bioorg Med Chem. 2016 Oct 1;24(19):4647-51. [Content Brief]

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Keywords:

AZ960905586-69-8AZ 960AZ-960JAKApoptosisParasiteVirus ProteaseJanus kinaseInhibitorinhibitorinhibit

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AZ960

Customer Review

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References

Customer Review

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