Utatrectinib

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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。

CAS NO:

1079274-94-4

AZD-7451

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.