Lestaurtinib
Cat. No.：YN340239
CAS No. ：111358-88-4
| 产品名称: | Lestaurtinib |
| CAS No.: | 111358-88-4 |
| Chemical Name: | 2,3,9S,10S,11,12R-hexahydro-10-hydroxy-10-(hydroxymethyl)-9-methyl-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocin-1-one |
| Synonyms: | CEP-701; KT-5555 |
| 分子量: | 439.46 |
| 分子式: | C₂₆H₂₁N₃O₄ |
| SMILES: | O=C(NC1)C2=C1C3=C(C4=C52)N(C6=C3C=CC=C6)[C@@]([C@@](O)(CO)C7)(C)O[C@H]7N4C8=C5C=CC=C8 |
| 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: | Lestaurtinib (CEP-701;KT-5555) 是一种多激酶抑制剂，对Trk受体酪氨酸激酶家族具有强大的活性。 Lestaurtinib抑制JAK2，FLT3和TrkA的IC50分别为0.9，3，小于25 nM。 |
| IC50和靶点: | [{name:"JAK2:0.9 nM (IC50)"},{name: "TrkA:25 nM (IC50)"},{name: "FLT3:2 nM (IC50)"}] |
| In Vitro: | |
| In Vivo: | |
| Clinical Trial: | |
| Solvent & Solubility: |
Leonard, W.J., and O'Shea, J.J.JAKS AND STATS: Biological implicationsAnnu. Rev. Immunol.16,293-322(1998)
Yamaoka, K., Saharinen, P., Pesu, M., et al.The Janus kinases (Jaks)Genome Biol.5(12),253(2004)
Verstovsek, S.Therapeutic potential of JAK2 inhibitorsHematology Am. Soc. Hematol. Educ. Program,636-642(2009)
Hexner, E.O., Serdikoff, C., Jan, M., et al.Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disordersBlood111(12),5663-5671(2008)
Miknyoczki, S.J., Chang, H., Klein-Szanto, A., et al.The Trk tyrosine kinase inhibitor CEP-701 (KT-5555) exhibits significant antitumor efficacy in preclinical xenograft models of human pancreatic ductal adenocarcinomaClin. Cancer Res.5,2205-2212(1999)
Iyer, R., Evans, A.E., Qi, X., et al.Lestaurtinib enhances the anti-tumor efficacy of chemotherapy in murine xenograft models of neuroblastomaClin. Cancer Res.16(5),1478-1485(2010)
Diaz, T., Navarro, A., Ferrer, G., et al.Lestaurtinib inhibition of the JAK/STAT signaling pathway in Hodgkin lymphoma inhibits proliferation and induces apoptosisPLoS One6(4),(2011)
Köhler, J., Erlenkamp, G., Eberlin, A., et al.Lestaurtinib inhibits histone phosphorylation and androgen-dependent gene expression in prostate cancer cellsPLoS One7(4),(2012)
