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Submit ReviewNVP BSK 805 is a potent JAK2 inhibitor (IC50 = 0.48 nM). Exhibits >20-fold selectivity for JAK2 over TYK2, JAK3 and JAK1 (IC50 values are 10.8, 18.7 and 31.6 nM, respectively). Inhibits proliferation and induces apoptosis of JAK2V617F-bearing acute myeloid leukemia cells in vitro and in vivo. Also inhibits erythropoietin-induced polycythemia. Orally bioavailable.
NVP BSK 805 is also offered as part of the Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
| 分子量 | 599.94 |
| 公式 | C27H28F2N6O.3HCl |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 2320258-95-3 |
| PubChem ID | 131648244 |
| InChI Key | VWBSZLCFZWKXHV-UHFFFAOYSA-N |
| Smiles | FC1=C(CN2CCOCC2)C(F)=CC(C3=C4C(N=CC(C5=CN(C6CCNCC6)N=C5)=N4)=CC=C3)=C1.Cl.Cl.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
Baffert et al (2010) Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805. Mol.Cancer Ther. 9 1945 PMID: 20587663
Pissot-Soldermann et al (2010) Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors. Bioorg.Med.Chem.Lett. 20 2609 PMID: 20231096
关键词: NVP BSK 805, NVP BSK 805 supplier, NVPBSK805, JAK2, inhibitors, inhibits, potent, orally, bioavailable, AML, acute, myeloid, leukemia, polycythemia, JAK, Kinase, 5818, Tocris Bioscience
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