XL228
Cat. No.:YN440342
产品名称: | XL228 |
CAS No.: | 898280-07-4 |
Chemical Name: | N4-(5-cyclopropyl-1H-pyrazol-3-yl)-N2-[[3-(1-methylethyl)-5-isoxazolyl]methyl]-6-(4-methyl-1-piperazinyl)-2,4-pyrimidinediamine |
Synonyms: | XL228; XL 228 |
分子量: | 437.54 |
分子式: | C₂₂H₃₁N₉O |
SMILES: | CN1CCN(C2=CC(NC3=NNC(C4CC4)=C3)=NC(NCC5=CC(C(C)C)=NO5)=N2)CC1 |
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: | XL228是多靶点的酪氨酸激酶抑制剂,对Bcr-Abl,Aurora A,IGF-1R,Src和Lyn的IC50值分别为5,3.1,1.6,6.1,2 nM。 |
IC50和靶点: | [{name:"Aurora A:3.1 nM (IC50)"},{name: "IGF-1R:1.6 nM (IC50)"}] |
In Vitro: | |
In Vivo: | |
Clinical Trial: | |
Solvent & Solubility: |
Cortes, J., Paquette, R., Talpaz, M., et al.Preliminary clinical activity in a phase I trial of the BCR-ABL/IGF-1R/aurora kinase inhibitor XL228 in patients with Ph++ leukemias with either failure to multiple TKI therapies or with T315I mutationBlood112(11),3232(2008)
Clary, D.O., Ollmann, M.M., Detmer, S.A., et al.Abstract C192: Characterization of the target profile of XL228, a multi‐targeted protein kinase inhibitor in phase 1 clinical developmentMol. Cancer. Ther.8(12 Suppl),C192(2009)
Shah, N.P., Kasap, C., Paquette, R., et al.Targeting drug-resistant CML and Ph+-ALL with the spectrum selective protein kinase inhibitor XL228Blood110(11),474(2007)