2. Neuronal Signaling Protein Tyrosine Kinase/RTK
  3. Trk Receptor
  4. TIY-7

TIY-7 是一种选择性和具有口服活性的 原肌球蛋白受体激酶 (TRK) 抑制剂。TIY-7 对 TRKA, TRKAG595R, TRKAG667C, TRKAF589L, TRKCG623R, TRKCG696A 酶均显示出抑制活性其 IC50 值分别为 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM。TIY-7 在小鼠异种移植模型中显示出抗肿瘤效力。

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TIY-7 Chemical Structure

TIY-7 Chemical Structure

CAS No. : 2846435-83-2

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TIY-7 相关抗体

Top Publications Citing Use of Products

查看 Trk Receptor 亚型特异性产品:

查看所有亚型
TrkA TrkB TrkC Trk

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TIY-7 is a selective and orally active tropomyosin receptor kinase (TRK) inhibitor. TIY-7 shows enzyme inhibitory activity with IC50s of 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM for TRKA, TRKAG595R, TRKAG667C, TRKAF589L, TRKCG623R, TRKCG696A, respectively. TIY-7 shows anti-tumor potency in mouse xenograft model[1].

IC50 & Target[1]

TrkA

2.9 nM (IC50)

TrkA

 

TrkC

 

体外研究
(In Vitro)

TIY-7 (compound 12c) shows enzyme inhibitory activity with IC50s of 2.9, 1.1, 0.7, 0.8, 0.8, 0.2 nM for TRKA, TRKAG595R, TRKAG667C, TRKAF589L, TRKCG623R, TRKCG696A, respectively[1].
TIY-7 (1 µM) shows selectivity with inhibitory rate of 62%, 99%, 11% for ALK, ROS1, and JAK1 kinase[1].

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

TIY-7 相关抗体:
体内研究
(In Vivo)

TIY-7 (5 mg/kg for p.o.; 1 mg/kg for i.v.) shows good oral bioavailability (F) of 39.8%[1].
TIY-7 (30 mg/kg; P.o.; twice daily for 12-14 consecutive days) inhibits tumor progression in a dose-dependent manner in xenograft model[1].
Pharmacokinetic Parameters of TIY-7 in Male Sprague-Dawley rats[1].

Dose (mg/kg) Cmax (ng/mL) Tmax (h) T1/2 (h) CL (mL/min/kg) F % MRT0-t (h) AUCtot (ng/mL·h) AUCextra (%)
ip mice 9.103 2078 0.0833 0.8 154 86 0.7 982.3 1.3
iv mice 0.711 322.7 0.0833 1.1 133 0.9 88.8 15.2
iv dog 26.76 272 (µg/mL) 0.0833 3.8 0.69 3.8 654.7 (µg/mL·h) 0.9
Male Sprague-Dawley rats; 5 mg/kg for p.o.; 1 mg/kg for i.v.[1].

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

Animal Model: Male Sprague-Dawley rats[1]
Dosage: 5 mg/kg for p.o.; 1 mg/kg for i.v.
Administration: P.o. or i.v.
Result: Showed good PK properties with an oral bioavailability (F) of 39.8%.
Animal Model: 6-week-old BALB/cA nude mice (BaF3-TMP3-TRKA-WT and BaF3-ETV6-TRKC-G623R xenograft models)[1]
Dosage: 30 mg/kg (dissolved in 70% PEG400 and 30% water)
Administration: P.o.; twice daily; 12-14 consecutive days
Result: Dose-dependently inhibited tumor progression with the TGI of 95% and 86% in BaF3-TMP3-TRKA-WT and BaF3-ETV6-TRKC-G623R xenograft model.
分子量

446.40

Formula

C21H18F4N6O
CAS 号
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.
纯度 & 产品资料
参考文献

TIY-7 相关分类

  • 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.

Keywords:

TIY-72846435-83-2TIY7TIY 7Trk ReceptorTropomyosin related kinase receptordrug-resistanceanticancerBaF3-ETV6-TRKC-G623Rxenograft modelorally activeselectiveInhibitorinhibitorinhibit

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