Tuspetinib
Cat. No.:YN270711
CAS No. :2294874-49-8
产品名称: | Tuspetinib |
CAS No.: | 2294874-49-8 |
Chemical Name: | rel-5-chloro-N-[3-cyclopropyl-5-[[(3R,5S)-3,5-dimethyl-1-piperazinyl]methyl]phenyl]-4-(6-methyl-1H-indol-3-yl)-2-pyrimidinamine |
Synonyms: | HM43239 |
分子量: | 501.06546 |
分子式: | C29H33ClN6 |
SMILES: | ClC1=CN=C(NC2=CC(C3CC3)=CC(CN4C[C@H](N[C@H](C4)C)C)=C2)N=C1C5=CNC6=CC(C)=CC=C56 |
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: | Tuspetinib (HM43239) 是具有口服活性的选择性FLT3抑制剂,IC50值为 1.1 nM (FLT3 野生型)、1.8 nM (FLT3 ITD 突变型) 和 1.0 nM (FLT3 D835Y 突变型)。Tuspetinib 作为可逆的 I 型抑制剂直接抑制FLT3的激酶活性,并调节 p-STAT5, p-ERKSYK, JAK1/2 和 TAK1。Tuspetinib 抑制白血病细胞的增殖,诱导细胞凋亡 (apoptosis)。 |
IC50和靶点: | [{name:"FLT3 WT:1.1 nM (IC50)"},{name: "FLT3 ITD:1.8 nM (IC50)"},{name: "FLT3 D835Y:1.0 nM (IC50)"}] |
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Bae, I.H., Kim, J.S., Choi, J.Y., et al.Pyrimidine compounds and pharmaceutical compositions for preventing or treating cancers including the sameUS 10,870,639 B2,(2020)