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AdipoGen Life Sciences
AZ 960
80
CHF
CHF 80.00
In stock
AG-CR1-3752-M0011 mgCHF 80.00
AG-CR1-3752-M0055 mgCHF 240.00
AG-CR1-3752-M02525 mgCHF 840.00
| Product Details | |
|---|---|
| Synonyms | AZ960 |
| Product Type | Chemical |
| Properties | |
| Formula |
C18H16F2N6 |
| MW | 354.4 |
| CAS | 905586-69-8 |
| Purity Chemicals | ≥98% (HPLC) |
| Appearance | White to off-white solid. |
| Solubility | Soluble in DMSO (20mg/ml), DMF (20mg/ml) or ethanol (2mg/ml). |
| Identity | Determined by 1H-NMR |
| InChi Key | SUNXHXDJOIXABJ-NSHDSACASA-N |
| Smiles | FC1=C(NC2=NNC(C)=C2)N=C(N[C@@H](C)C3=CC=C(F)C=C3)C(C#N)=C1 |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Keep cool and dry. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- AZ-960 is a potent, selective and ATP-competitive JAK2 inhibitor that inhibits JAK2 kinase with a Ki of 0.45nM in vitro (3-fold selective over JAK3) and induces growth arrest and apoptosis in adult T cell leukemia (ATL) cells. Janus-associated kinases (JAKs) are cytoplasmic tyrosine kinases that are required for activating the signaling of certain cytokines and growth factor receptors. Many myeloproliferative diseases have been linked to a mutation in JAK2, where a switch from valine to phenylalanine occurs at position 617 (V617F). Furthermore, constitutive activation of the JAK2 signaling pathway is associated with aggressive adult T cell leukemia/lymphoma.
- AZ-960 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. It can decrease STAT3/5 phosphorylation and inhibit cell proliferation in a SET-2 human megakaryoblastic cell line that is heterozygous for the JAK2 V617F mutation with a GI50 value of 33 nM.
- AZ-960 shows anti-parasitic activity through selective inhibition of the Trypanosoma brucei ERK8 inhibitor (TbERK8).
Product References
- Effects of the JAK2 inhibitor, AZ960, on Pim/BAD/BCL-xL survival signaling in the human JAK2 V617F cell line SET-2: J.M. Gozgit, et al.; J. Biol. Chem. 283, 32334 (2008)
- AZ960, a novel Jak2 inhibitor, induces growth arrest and apoptosis in adult T-cell leukemia cells: J. Yang, et al.; Mol. Cancer Ther. 9, 3386 (2010)
- Expression of p-JAK2 predicts clinical outcome and is a potential molecular target of acute myelogenous leukemia: T. Ikezoe, et al.; Int. J. Cancer 129, 2512 (2011)
- Discovery and antiparasitic activity of AZ960 as a Trypanosoma brucei ERK8 inhibitor: A.L. Valenciano, et al.; Bioorg. Med. Chem. 24, 4647 (2016)
- Phenotypic Screen Identifies JAK2 as a Major Regulator of FAT10 Expression: N. Reznik, et al.; ACS Chem. Biol. 14, 2538 (2019)
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