Cat. No. Name Size Price Add Cart
KI0269AZD14805 mg$160
AZD148010 mg$272
AZD148050 mg$912
AZD1480200 mg$2512

Chemical Characteristic

Product NameAZD1480
CAS No.935666-88-9
Molecular Weight 348.77
FormulaC14H14ClFN8
Chemical Name(S)-5-chloro-N2-(1-(5-fluoropyrimidin-2-yl)ethyl)-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine
Smilesc1(nc(c(cn1)Cl)Nc1n[nH]c(c1)C)N[C@@H](C)c1ncc(cn1)F
Chemical Structure

Biological activities

AZD1480 is a potent ATP competitive inhibitor of JAK2 kinase, with an inhibition constant (Ki) of 0.26 nM. AZD1480 has significant JAK2 selectivity over JAK3, enzymatic assays at Km levels of ATP shows the IC50s JAK1, JAK2, and JAK3 are 1.3, <0.4 and 3.9 nM, respectively, while at high end of ATP concentrations of 5 mM, the enzyme IC50 are 41, 58 nM, and 1.36 µM for JAK1, JAK2, and JAK3, respectively. [1] AZD1480 inhibits the phosphorylation of Stat5 with an IC50 of 46 nM in TEL-JAK2 cells. Meanwhile, AZD1480 potently inhibits the growth of the TEL-JAK2 cell line with a GI50 of 60 nM. [1] AZD1480 inhibits U266 cells and Kms.11 cells proliferation at 48 hours with IC50 values of approximately 2 and 1 µM, respectively. At 72 hours, the IC50s are approximately 1 and 0.5 µM. IL-6-induced phosphorylation of JAK2 is inhibited by AZD1480 at 0.25-0.5 µM and virtually abolished at 1 µM in both U266 and Kms.11 cells. In vitro, AZ1480 inhibits both JAK2 and FGFR3 activity, consistent with role of JAK2/STAT3 and FGFR3 in the biological effects mediated by AZD1480. [2] AZD1480 at low doses (0.1?? mM) inhibits constitutive STATs phosphorylation in HL cell lines, demonstrating immunoregulatory effects as it downregulated the surface expression of the STAT3-target immunosuppressive cell-surface protein PD-L1 and PD-L2, in addition to downregulation of IL-13, IL-6 and TARC. [3] In vivo, AZD1480 blocks proliferation, survival, FGFR3 and JAK/STAT3 signaling in myeloma cells cultured alone or cocultured with bone marrow stromal cells. AZD1480, twice a day with 30 mg/kg, inhibits significantly tumor growth in NOD/SCID IL2Rγ-null mice. [2]

Protocols

AZD1480 is dissolved in 100 % DMSO to prepare a 10 mM stock and stored at -20 °C. [2]

References

[1] Hedvat M, et al. The JAK2 Inhibitor AZD1480 Potently Blocks Stat3 Signaling and Oncogenesis in Solid Tumors. Cancer Cell. 2009, 16: 487??97.
[2] Scuto A, et al. The novel JAK inhibitor AZD1480 blocks STAT3 and FGFR3 signaling, resulting in suppression of human myeloma cell growth and survival. Leukemia. 2011, 25: 538??50.
[3] Derenzini E, et al. The JAK inhibitor AZD1480 regulates proliferation and immunity in Hodgkin lymphoma. Blood Cancer J. 2011, 1: 1-11.

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