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AZD1480

Cat. No. M2044
AZD1480 Structure
Size Price Availability Quantity
10mg USD 130 In stock
50mg USD 390 In stock
100mg USD 650 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

AZD1480 is a potent JAK2 inhibitor with an IC50 of 0.26 nM. AZD1480 inhibits constitutive and stimulus-induced phosphorylation of JAK2 and STAT-3 in vitro, downstream gene expression, and inhibits cell proliferation. AZD1480 suppresses STAT-3 activation in the glioma-initiating cell population in glioblastoma (GBM) tumors. In vivo, AZD1480 inhibits the growth of subcutaneous tumors and increases survival of mice bearing intracranial GBM tumors by inhibiting STAT-3 activity. Importantly, AZD1480 induces cell death of Kms.11 cells grown in the presence of HS-5 bone marrow (BM)-derived stromal cells and inhibits tumor growth in a Kms.11 xenograft mouse model, accompanied with inhibition of phospho-FGFR3, phospho-JAK2, phospho-STAT3 and Cyclin D2 levels. AZD1480 blocks proliferation, survival, FGFR3 and JAK/STAT3 signaling in myeloma cells cultured alone or cocultured with BM stromal cells, and in vivo, and leads to a decrease in cell proliferation and induction of apoptosis.

Protocol
Cell Experiment
Cell lines Renca or 786-O cells
Preparation method Cell viability assay.
Renca or 786-O cells suspended in DMEM medium with 5% FBS were seeded in 96-well plates (5,000 per well) to allow adhesion and then treated with DMSO or AZD1480 for 48 h. Cell viability was determined by MTS assay (Promega, Madison, WI) according to instructions. Absorbance at 490 nm was measured with Mikrotek Laborsysteme (Overath, Germany). Mouse ECs and splenic CD11b+/c− myeloid cells enriched from tumor bearing mice were cultured in 5% FBS 1640 RPMI medium. HUVECs were cultured on collagen 1-coated plates in complete medium (Clonetics). All cells are treated with DMSO and AZD1480 at various doses for 24 h. Cell viability was determined by counting cell number manually. All the experiments were repeated 3 times.
Concentrations 0, 0.1, 0.5, 1.0, 2.5, and 5 μM
Incubation time 48 h
Animal Experiment
Animal models Female BALB/c and athymic nude (NCR-nu/nu) mice (7-8 weeks old)
Formulation water supplemented with 0.5% Hypromellose and 0.1% Tween 80
Dosages 50 mg/kg once a day or 30 mg/kg twice daily for 21 days
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 348.77
Formula C14H14ClFN8
CAS Number 935666-88-9
Purity >99%
Solubility DMSO 65 mg/mL
Storage at -20°C
References

The JAK inhibitor AZD1480 regulates proliferation and immunity in Hodgkin lymphoma.
Derenzini E, et al. Blood Cancer J. 2011 Dec;1(12):e46. PMID: 22829094.

Therapeutic potential of AZD1480 for the treatment of human glioblastoma.
McFarland BC, et al. Mol Cancer Ther. 2011 Dec;10(12):2384-93. PMID: 22027691.

Antiangiogenic and antimetastatic activity of JAK inhibitor AZD1480.
Xin H, et al. Cancer Res. 2011 Nov 1;71(21):6601-10. PMID: 21920898.

The novel JAK inhibitor AZD1480 blocks STAT3 and FGFR3 signaling, resulting in suppression of human myeloma cell growth and survival.
Scuto A, et al. Leukemia. 2011 Mar;25(3):538-50. PMID: 21164517.

The JAK2 inhibitor AZD1480 potently blocks Stat3 signaling and oncogenesis in solid tumors.
Hedvat M, et al. Cancer Cell. 2009 Dec 8;16(6):487-97. PMID: 19962667.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AZD1480 supplier, JAK, inhibitors

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