Free shipping on all orders over $ 500

AZD1480

Cat. No. M2044
AZD1480 Structure
Synonym:

AZD1480; AZD 1480

Size Price Availability Quantity
10mg USD 80  USD80 In stock
50mg USD 200  USD200 In stock
100mg USD 350  USD350 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • 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.

Product Citations
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 348.77
Formula C14H14ClFN8
CAS Number 935666-88-9
Purity >98%
Solubility DMSO 65 mg/mL
Storage at -20°C
References

[1] Derenzini E, et al. Blood Cancer J. The JAK inhibitor AZD1480 regulates proliferation and immunity in Hodgkin lymphoma.

[2] McFarland BC, et al. Mol Cancer Ther. Therapeutic potential of AZD1480 for the treatment of human glioblastoma.

[3] Xin H, et al. Cancer Res. Antiangiogenic and antimetastatic activity of JAK inhibitor AZD1480.

[4] Scuto A, et al. Leukemia. The novel JAK inhibitor AZD1480 blocks STAT3 and FGFR3 signaling, resulting in suppression of human myeloma cell growth and survival.

[5] Hedvat M, et al. Cancer Cell. The JAK2 inhibitor AZD1480 potently blocks Stat3 signaling and oncogenesis in solid tumors.

Related JAK Products
BMS-986202

BMS-986202 is a potent, selective, orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC50 of 0.19 nM and a Ki of 0.02 nM. BMS-986202 is also a weak inhibitor of CYP2C19 with an IC50 of 14 μM. BMS-986202 can be used in IL-23-driven echinococcosis BMS-986202 can be used in studies of IL-23-driven echinococcosis, anti-CD40-induced colitis and spontaneous lupus.

GDC046

GDC046 (Compound 3) is a potent, selective, and orally bioavailable inhibitor of TYK2 with Ki of 4.8 nM, 83.8 nM, 27.6 nM and 253 nM for TYK2, JAK1, JAK2, and JAK3, respectively.

RO495

RO495 (CS-2667) is a potent inhibitor of Non-receptor tyrosine-protein kinase 2 (TYK2).

TG-89

TG-89 is a JAK inhibitor that inhibits JAK2, FLT3, RET and JAK3.

WYE-175765

WYE-175765 is a JAK3 and YopH inhibitor

  Catalog
Abmole Inhibitor Catalog




Keywords: AZD1480, AZD1480; AZD 1480 supplier, JAK, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.