AZ-960
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MedKoo CAT#: 406191

CAS#: 905586-69-8

Description: AZ960 is a novel inhibitor of Jak2 kinase. AZ960 inhibits JAK2 kinase with a K(i) of 0.00045 microm in vitro and treatment of TEL-JAK2 driven Ba/F3 cells with AZ960 blocked STAT5 phosphorylation and potently inhibited cell proliferation (GI(50)=0.025 microm). AZ960 demonstrated selectivity for TEL-JAK2-driven STAT5 phosphorylation and cell proliferation when compared with cell lines driven by similar fusions of the other JAK kinase family members.


Chemical Structure

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AZ-960
CAS# 905586-69-8

Theoretical Analysis

MedKoo Cat#: 406191
Name: AZ-960
CAS#: 905586-69-8
Chemical Formula: C18H16F2N6
Exact Mass: 354.14045
Molecular Weight: 354.36
Elemental Analysis: C, 61.01; H, 4.55; F, 10.72; N, 23.72

Price and Availability

Size Price Availability Quantity
5.0mg USD 150.0 Same Day
10.0mg USD 250.0 Same Day
25.0mg USD 450.0 Same Day
50.0mg USD 750.0 Same Day
100.0mg USD 1150.0 Same Day
200.0mg USD 1950.0 Same Day
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Synonym: AZ960; AZ 960; AZ-960.

IUPAC/Chemical Name: (S)-5-fluoro-2-(1-(4-fluorophenyl)ethylamino)-6-(5-methyl-1H-pyrazol-3-ylamino)nicotinonitrile

InChi Key: SUNXHXDJOIXABJ-NSHDSACASA-N

InChi Code: InChI=1S/C18H16F2N6/c1-10-7-16(26-25-10)23-18-15(20)8-13(9-21)17(24-18)22-11(2)12-3-5-14(19)6-4-12/h3-8,11H,1-2H3,(H3,22,23,24,25,26)/t11-/m0/s1

SMILES Code: N#CC1=C(N[C@H](C2=CC=C(F)C=C2)C)N=C(NC3=NNC(C)=C3)C(F)=C1

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >5 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Biological target: AZ960 is a potent and specific inhibitor of the JAK2 kinase with a Ki of 0.45 nM.
In vitro activity: AZ960, a novel inhibitor of Jak2 kinase, effectively induced 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. Interestingly, AZ960 increased levels of Bcl-xL in MT-1 and MT-2 cells in association with accumulation of cAMP response element-binding protein bound to the Bcl-xL promoter as measured by chromatin immunoprecipitation assay. Importantly, genetic inhibition of Bcl-xL by a small interfering RNA potentiated antiproliferative effects of AZ960 in MT-1 cells. Reference: Mol Cancer Ther. 2010 Dec;9(12):3386-95. http://mct.aacrjournals.org/cgi/pmidlookup?view=long&pmid=21159615

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 30.0 84.66

Preparing Stock Solutions

The following data is based on the product molecular weight 354.36 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
In vitro protocol: 1. Yang J, Ikezoe T, Nishioka C, Furihata M, Yokoyama A. 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. doi: 10.1158/1535-7163.MCT-10-0416. PMID: 21159615. 2. Gozgit JM, Bebernitz G, Patil P, Ye M, Parmentier J, Wu J, Su N, Wang T, Ioannidis S, Davies A, Huszar D, Zinda M. 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. doi: 10.1074/jbc.M803813200. Epub 2008 Sep 4. PMID: 18775810.

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1: Ikezoe T, Kojima S, Furihata M, Yang J, Nishioka C, Takeuchi A, Isaka M, Koeffler HP, Yokoyama A. 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. doi: 10.1002/ijc.25910. Epub 2011 Apr 8. PubMed PMID: 21207414.

2: Yang J, Ikezoe T, Nishioka C, Furihata M, Yokoyama A. 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. doi:  10.1158/1535-7163.MCT-10-0416. PubMed PMID: 21159615.

3: Gozgit JM, Bebernitz G, Patil P, Ye M, Parmentier J, Wu J, Su N, Wang T, Ioannidis S, Davies A, Huszar D, Zinda M. 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. doi: 10.1074/jbc.M803813200. Epub 2008 Sep 4. PubMed PMID: 18775810.

AZ-960

5.0mg / USD 150.0


Additional Information