2. Neuronal Signaling Protein Tyrosine Kinase/RTK
  3. Trk Receptor
  4. TRK-IN-31

TRK-IN-31 是一种口服有效的 TRK 抑制剂，IC50 为 1.8 nM。TRK-IN-31 在 Ba/F3-MPRIP-TRKAG667C 细胞中表现出优异的抗增殖活性，并能高选择性地有效抑制 TRK 激酶活性。TRK-IN-31 显著抑制 Ba/F3-MPRIP-TRKAG667C 皮下肿瘤小鼠模型中的肿瘤生长。

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TRK-IN-31 Chemical Structure

TRK-IN-31 Chemical Structure

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Other Forms of TRK-IN-31:

TRK-IN-31 相关抗体

Top Publications Citing Use of Products

查看 Trk Receptor 亚型特异性产品:

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TrkA TrkB TrkC Trk

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TRK-IN-31 is an orally active TRK inhibitor with an IC50 of 1.8 nM. TRK-IN-31 has superior antiproliferative activity in the Ba/F3-MPRIP-TRKAG667C cells, and potently inhibits TRK kinase activity with high selectivity. TRK-IN-31 significantly inhibits tumor growth in Ba/F3-MPRIP-TRKAG667C subcutaneous tumor mice model[1].

IC50 & Target

TRK

1.8 nM ()

体外研究
(In Vitro)

TRK-IN-31 (Compound 10o) (72 小时) 具有强效的抗增殖活性，对 Ba/F3-MPRIP-TRKAG667C 细胞和 Ba/F3-MPRIP-TRKAG595R 细胞的 IC50 分别为 81.4 nM 和 131.4 nM[1]。
TRK-IN-31 (1-20 nM，2 小时) 显著抑制 Ba/F3-MPRIP-TRKA 和 MO-91 细胞中的 TRK 信号传导[1]。
TRK-IN-31 (0.04-1 μM，2 小时) 显著抑制 Ba/F3-MPRIP-TRKAG667C 细胞中 TRKA G667C 信号传导，在 0.2 μM 浓度下效果更显著[1]。
TRK-IN-31 (1 μM，1 小时) 在 92 种激酶 (S(10): 0.043) 中具有较高的选择性，对 TRKA/B/C 和 CSF1R 具有显著的抑制活性，抑制率为 97%-103%[1]。
TRK-IN-31 对 TRKAG595R 具有优异的结合能力，增强了与蛋白质的稳定性，并减少了构象波动[1]。

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

TRK-IN-31 相关抗体:

Western Blot Analysis[1]

Cell Line: Ba/F3-MPRIP-TRKA cells, MO-91 cells
Concentration: 1, 5, 20 nM
Incubation Time: 2 h
Result: Notably inhibited TRK signaling in both Ba/F3-MPRIP-TRKA and MO-91 cells.
Nearly abolished the activation of TRKA and its key downstream molecules PLCγ and Erk at 5 nmol/L in Ba/F3-MPRIP-TRKA cells.
体内研究
(In Vivo)

TRK-IN-31 (Compound 10o) (25-150 mg/kg，口服，每日两次，连续 10 天) 在 Ba/F3-MPRIP-TRKAG667C 皮下肿瘤小鼠模型中具有强效的抗肿瘤活性，并呈剂量依赖性，且高达 150mg/kg 的剂量下仍具有良好的耐受性[1]。

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

Animal Model: Female nude mice (4-6 weeks old) were injected subcutaneously into the right flank with Ba/F3-MPRIP-TRKAG667C cells (2 × 106 cells/mouse)[1].
Dosage: 25, 150 mg/kg
Administration: Oral gavage (p.o.), twice daily for 10 days after tumors reaching approximately 50 mm3.
Result: Significantly delayed tumor growth in a dose-dependent manner, with inhibition rates of 42.4% and 52.5% at 25 and 150 mg/kg, respectively.
Had good tolerance with no significant body weight loss up to 150 mg/kg.
分子量

561.58

Formula

C30H29F2N5O4
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

TRK-IN-31 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:

TRK-IN-31Trk ReceptorTropomyosin related kinase receptorInhibitorsAntitumorBa/F3-MPRIP-TRKAG667C subcutaneous tumor mice modelBa/F3-MPRIP-TRKAG595R cellsBa/F3-MPRIP-TRKAG667C cellsInhibitorinhibitorinhibit

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产品名称：
TRK-IN-31
目录号：
HY-174330
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