1. Neuronal Signaling Protein Tyrosine Kinase/RTK
  2. Trk Receptor
  3. Utatrectinib

Utatrectinib  (Synonyms: AZD-7451)

目录号: HY-102066 纯度: 98.72%
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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。

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Utatrectinib Chemical Structure

Utatrectinib Chemical Structure

CAS No. : 1079274-94-4

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查看 Trk Receptor 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Utatrectinib (AZD-7451) is a potent, selective and orally active Trk inhibitor. Utatrectinib blocks TrkC activation 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
性状

固体

颜色

Blue to blue-green

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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