XL019
Cat. No.：YN340147
CAS No. ：945755-56-6
| 产品名称: | XL019 |
| CAS No.: | 945755-56-6 |
| Chemical Name: | (2S)-N-[4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]phenyl]-2-pyrrolidinecarboxamide |
| Synonyms: | XL019; XL-019; XL 019. |
| 分子量: | 444.53 |
| 分子式: | C₂₅H₂₈N₆O₂ |
| SMILES: | O=C([C@H]1NCCC1)NC2=CC=C(C3=NC(NC4=CC=C(N5CCOCC5)C=C4)=NC=C3)C=C2 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | XL019 是一种有效的、口服活性的、选择性的JAK2抑制剂，对 JAK2，JAK1，JAK3 的IC50分别为 2.2、134.3、214.2 nM。XL019 对JAK2的选择性是 100 多种丝氨酸/苏氨酸和酪氨酸激酶（包括 JAK 家族的其他成员）的 50 倍或更高。XL019 对 JAK2 V617F 和野生型 JAK2 细胞中 STAT3 和 STAT5 磷酸化的抑制作用。 |
| IC50和靶点: | [{name:"JAK2:2.2 nM (IC50)"},{name: "JAK3:214.2 nM (IC50)"}] |
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| Solvent & Solubility: |
Gozgit, J.M., Bebernitz, G., Patil, P., et al.Effects of the JAK2 inhibitor, AZ960, on Pim/BAD/BCL-xL survival signaling in the human JAK2 V617F cell line SET-2J. Biol. Chem.283(47),32334-32343(2008)
Yang, J., Ikezoe, T., Nishioka, C., et al.AZ960, a novel Jak2 inhibitor, induces growth arrest and apoptosis in adult T-cell leukemia cellsMol. Cancer Ther.9(12),3386-3395(2010)
Forsyth, T., Kearney, P.C., Kim, B.G., et al.SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitorsBioorg. Med. Chem. Lett.22(24),7653-7658(2012)
Verstovsek, S.Therapeutic potential of JAK2 inhibitorsHematology Am. Soc. Hematol. Educ. Program,636-642(2009)
Furqan, M., Mukhi, N., Lee, B., et al.Dysregulation of JAK-STAT pathway in hematological malignancies and JAK inhibitors for clinical applicationBiomark. Res.1(1),5(2013)
