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Utatrectinib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Utatrectinib图片
CAS NO:1079274-94-4
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
AZD-7451
产品介绍
Utatrectinib (AZD-7451) 是一种有效的、选择性的和具有口服活性的Trk抑制剂。Utatrectinib 可阻断 TrkC 激活和相关的致瘤行为。
生物活性

Utatrectinib (AZD-7451) is a potent, selective and orally activeTrkinhibitor. Utatrectinib blocksTrkCactivation and associated tumorigenic behaviors[1].

体外研究
(In Vitro)

Utatrectinib (100 nM, 22 h) inhibits the migration of TrkC-expressing U2SO cells[2].
Utatrectinib (1-10 nM, 24 h) inhibits cell growth in KM12, H460 and H810 cells[3].
Utatrectinib (5 nM, 24 h) inhibits phosphorylation of TRKA/B and downstream signaling in KM12, H460 cells[3].

Cell Migration Assay[2]

Cell Line:TrkC-expressing U2SO cells
Concentration:100 nM
Incubation Time:22 h
Result:Inhibited cell migration (~2.3-fold, P<0.01).

Western Blot Analysis[3]

Cell Line:KM12, H460 cells
Concentration:0, 1, 5 nM
Incubation Time:24 h
Result:Inhibited pTRKA Tyr490 and pAk in KM12 cells.
Inhibited pTRKB Tyr706/707 and pERK in H460 cells.
体内研究
(In Vivo)

Utatrectinib (50 mg/kg, p.o., daily) suppresses adenoid cystic carcinoma (ACC) tumor growth in ACCX6 xenograft nu/nu mice model[2].

Animal Model:Xenograft nu/nu mice models of human ACC: ACCX6 and ACCX9[2]
Dosage:50 mg/kg
Administration:Oral administration, daily.
Result:Tumor growth inhibition (TGI): 64% (in ACCX6 model)
Clinical Trial
分子量

382.39

Formula

C18H19FN8O

CAS 号

1079274-94-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.