AZ 960
| Code | Size | Price |
|---|
| AG-CR1-3752-M001 | 1 mg | £70.00 |
Quantity:
| AG-CR1-3752-M005 | 5 mg | £190.00 |
Quantity:
| AG-CR1-3752-M025 | 25 mg | £640.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
AMBIENT
Storage:
Short Term: +4°C Long Term: -20°C
Documents
Further Information
Alternate Names/Synonyms:
AZ960
Appearance:
White to off-white solid.
CAS:
905586-69-8
EClass:
32160000
Form (Short):
liquid
Handling Advice:
Keep cool and dry.
InChi:
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/s1InChI=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
InChiKey:
SUNXHXDJOIXABJ-NSHDSACASA-N
Long Description:
Chemical. CAS: 905586-69-8. Formula: C18H16F2N6. MW: 354.4. 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).
MDL:
MFCD16621127
Molecular Formula:
C18H16F2N6
Molecular Weight:
354.4
Package Type:
Vial
Product 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).
Purity:
>95%
SMILES:
FC1=C(NC2=NNC(C)=C2)N=C(N[C@@H](C)C3=CC=C(F)C=C3)C(C#N)=C1
Solubility Chemicals:
Soluble in DMSO (20mg/ml), DMF (20mg/ml) or ethanol (2mg/ml).
Transportation:
Non-hazardous
UNSPSC Category:
Protein Kinase Modulators
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
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)