Biological Activity
Potent and selective JAK2 inhibitor (IC50 < 3 nM). Exhibits >50-fold selectivity for JAK2 over JAK3. Exhibits antitumor effects and inhibits formation of lung metastases in a mouse renal cancer model. Also inhibits STAT3 signaling, tumor angiogenesis and myeloid cell migration in vivo.
Compound Libraries
AZD 1480 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 348.77 |
| Formula | C14H14ClFN8 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 935666-88-9 |
| PubChem ID | 16659841 |
| InChI Key | PDOQBOJDRPLBQU-QMMMGPOBSA-N |
| Smiles | C[C@@H](C1=NC=C(F)C=N1)NC2=NC=C(Cl)C(NC3=NNC(C)=C3)=N2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 34.88 | 100 | |
| ethanol | 34.88 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 348.77. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.87 mL | 14.34 mL | 28.67 mL |
| 5 mM | 0.57 mL | 2.87 mL | 5.73 mL |
| 10 mM | 0.29 mL | 1.43 mL | 2.87 mL |
| 50 mM | 0.06 mL | 0.29 mL | 0.57 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Ioannidis S et al (2011) Discovery of 5-chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the Jak/Stat pathway. J.Med.Chem. 54 262 PMID: 21138246
Xin et al (2011) Antiangiogenic and antimetastatic activity of JAK inhibitor AZD1480. Cancer Res. 71 6601 PMID: 21920898
Keywords: AZD 1480, supplier, AZD1480, JAK2, inhibitors, cancer, anticancers, metastasis, angiogenesis, STAT3, signaling, potent, selective, inhibits, JAK, Kinase, Antiangiogenics, JAK, Kinase, Tocris Bioscience
