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Datasheet of AZD1480

Description:
AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM, selectivity against JAK3 and Tyk2, and to a smaller
extent against JAK1.
in vitro: AZD1480 demonstrated significant immunoregulatory effects by downregulating T-helper 2 cytokines and chemokines,
including IL-13 and thymus- and activation-regulated chemokine, and the surface expression of the immunosuppressive
programmed death ligands 1 and 2. Higher concentrations of AZD1480 (5) induced G2/M arrest and cell death by inhibiting
Aurora kinases. These biological responses to AZD1480 are associated with concomitant inhibition of phosphorylation of JAK2,
STAT3 and MAPK signaling proteins. In addition, there is inhibition of expression of STAT3 target genes, particularly Cyclin D2.
Examination of a wider variety of myeloma cells (RPMI 8226, OPM-2, NCI-H929, Kms.18, MM1.S and IM-9), as well as
primary myeloma cells, showed that AZD1480 has broad efficacy. AZD1480 treatment effectively blocks constitutive and
stimulus-induced JAK1, JAK2, and STAT-3 phosphorylation in both human and murine glioma cells, and leads to a decrease in
cell proliferation and induction of apoptosis. AZD1480 inhibits STAT3 in tumor-associated myeloid cells, reducing their number
and inhibiting tumor metastasis. Myeloid cell-mediated angiogenesis was also diminished by AZD1480, with additional direct
inhibition of endothelial cell function in vitro and in vivo.
in vivo: AZD1480 inhibits the STAT3 phosphorylation in an xenograft model of human solid tumors and multiple myeloma. n
vivo, AZD1480 inhibits the growth of subcutaneous tumors and increases survival of mice bearing intracranial glioblastoma
(GBM) tumors by inhibiting STAT-3 activity, indicating that pharmacologic inhibition of the JAK/STAT-3 pathway by AZD1480
should be considered for study in the treatment of patients with GBM tumors. AZD1480 blocks lung infiltration of myeloid cells
and formation of pulmonary metastases in both mouse syngeneic experimental and spontaneous metastatic models. Furthermore,
AZD1480 reduces angiogenesis and metastasis in a human xenograft tumor model .

Chemical Information
Catalog

DC5032

Purity of current batch:

>98%

Molecular Weight (MW)

348.77

Molecular Formula

C14H14ClFN8

CAS No.

935666-88-9

Solubility (25C)

DMSO

Storage

Store at -20C (desiccating conditions).

Handling:
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in
advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable
for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room
temperature for at least 1 hour.