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| 5-Chloro-N2-[(1S)-1-(5-fluoro-2-pyrimidinyl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)-2,4-pyrimidinediamine Basic information |
| Product Name: | 5-Chloro-N2-[(1S)-1-(5-fluoro-2-pyrimidinyl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)-2,4-pyrimidinediamine | | Synonyms: | 5-Chloro-N2-[(1S)-1-(5-fluoro-2-pyrimidinyl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)-2,4-pyrimidinediamine;AZD 1480;(S)-5-chloro-N4-(5-Methyl-1H-pyrazol-3-yl)-N2-(1-(5-MethylpyriMidin-2-yl)ethyl)pyriMidine-2,4-diaMine;(S)-5-chloro-N2-(1-(5-fluoropyriMidin-2-yl)ethyl)-N4-(5-Methyl-1H-pyrazol-3-yl)pyriMidine-2,4-diaMine;5-Chloro-N2-[(1S)-1-(5-fluoro-2-pyrimidinyl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)-2,4-pyrimidinediamine AZD 1480;5-Chloro-N2-[(1S)-1-(5-fluoro-2-pyrimidinyl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)-2,4-pyrimidine-2,4-diamine;AZD-1480;AZD 1480;AZD 1480 5-Chloro-N2-[(1S)-1-(5-fluoro-2-pyrimidinyl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)-2,4-pyrimidinediamine | | CAS: | 935666-88-9 | | MF: | C14H14ClFN8 | | MW: | 348.77 | | EINECS: | | Product Categories: | Inhibitors;JAK;Inhibitor;API;STAT | | Mol File: | 935666-88-9.mol |
| 5-Chloro-N2-[(1S)-1-(5-fluoro-2-pyrimidinyl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)-2,4-pyrimidinediamine Chemical Properties |
| Melting point | >205°C (dec.) | | Boiling point | 575.2±60.0 °C(Predicted) | | density | 1.517 | | storage temp. | -20°C | | solubility | Chloroform (Slightly, Heated), DMSO (Slightly, Heated), Methanol (Slightly, Heat | | pka | 13.73±0.10(Predicted) | | form | powder | | color | white to beige |
| 5-Chloro-N2-[(1S)-1-(5-fluoro-2-pyrimidinyl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)-2,4-pyrimidinediamine Usage And Synthesis |
| Uses | AZD1480 has been used as an inhibitor of janus kinase 2 (JAK2) and signal transducer and activator of transcription 3 (STAT3) in an in vitro cell model of upper gastrointestinal adenocarcinoma. It has also been used in combination with bortezomib to study tumor-associated macrophage-mediated survival of myeloma cells. | | Biological Activity | azd1480 is a novel small-molecule jak inhibitor. it is able to block cell proliferation and induce apoptosis of myeloma cell lines. it can effectively inhibit tumor angiogenesis and metastasis mediated by stat3 in stromal cells as well as tumor cells. azd1480 has broad efficacy on a wider variety of myeloma cells, such as rpmi 8226, opm-2, nci-h929, kms.18, mm1.s and im-9, as well as primary myeloma cells. 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 also demonstrates important jak2 selectivity over jak3, in particular at high atp concentrations and marginal selectivity over jak1 at km atp.a scuto, p krejci, l popplewell, j wu, y wang, m kujawski, c kowolik, h xin, l chen, y wang, l kretzner, h yu, w r wilcox, y yen, s forman and r jove. the novel jak inhibitor azd1480 blocks stat3 and fgfr3 signaling, resulting in suppression of human myeloma cell growth and survival. leukemia. 2011 march ; 25(3): 538–550michael hedvat, dennis huszar, andreas herrmann, joseph m. gozgit, anne schroeder, adam sheehy, ralf buettner, david proia, claudia m. kowolik, hong xin, brian armstrong, geraldine bebernitz, shaobu weng, lin wang, minwei ye, kristen mceachern, huawei chen, deborah morosini, kirsten bell, marat alimzhanov, stephanos ioannidis, patricia mccoon, zhu a. cao, hua yu, richard jove, michael zinda. the jak2 inhibitor azd1480 potently blocks stat3 signaling and oncogenesis in solid tumors. cancer cell. 2009; 16 (6): 487–497hong xin, andreas herrmann, karen reckamp, wang zhang, sumanta pal, michael hedvat, chunyan zhang, wei liang, anna scuto, shaobu weng, deborah morosini, zhu a. cao, michael zinda, robert figlin, dennis huszar, richard jove, hua yu. antiangiogenic and antimetastatic activity of jak inhibitor azd1480. cancer research. 2011;71: 6601-6610 | | Biochem/physiol Actions | AZD1480 is an orally active, potent and selective inhibitor of Janus kinases JAK1 and JAK 2 with selectivity for JAK2 as evidenced by IC50 values of 1.3 nM for JAK1 and <0.4 nM for JAK2 in enzyme assays. AZD1480 inhibits endogenous as well as IL-6 induced STAT3 activation. AZD1480 reduces myeloid cell-mediated angiogenesis and metastasis. AZD1489 is an effective anticancer agent in bot adult and pediatric human tumors. |
| 5-Chloro-N2-[(1S)-1-(5-fluoro-2-pyrimidinyl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)-2,4-pyrimidinediamine Preparation Products And Raw materials |
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