2. Neuronal Signaling Protein Tyrosine Kinase/RTK Apoptosis
  3. Trk Receptor Apoptosis
  4. TRK-IN-33

TRK-IN-33 是一种 TRK 抑制剂。TRK-IN-33 展现出优异的 TRKAG667C 降解能力 (DC50 = 24.69 nM；Dmax > 90%) 同时不影响野生型蛋白。TRK-IN-33 对携带 NTRK1G667C 的 Ba/F3-LMNA-NTRK1G667C 细胞具有抗增殖活性，IC50 值为 2.48 nM。TRK-IN-33 能在体内有效抑制肿瘤生长，诱导肿瘤细胞凋亡 (apoptosis) 且无明显毒性。TRK-IN-33 可用于 NTRK 融合阳性癌症的研究。

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TRK-IN-33

TRK-IN-33 Chemical Structure

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TRK-IN-33 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

TRK-IN-33 is a TRK inhibitor. TRK-IN-33 exhibits excellent TRKAG667C degradation (DC50 = 24.69 nM; Dmax > 90%), while sparing the wild-type protein in virto. TRK-IN-33 shows antiproliferative activities against Ba/F3-LMNA-NTRK1G667C cells with an IC50 value of 2.48 nM. TRK-IN-33 effectively inhibits tumor growth and enhances apoptosis in tumor tissues with no apparent toxicity in vivio. TRK-IN-33 can be used for NTRK fusion−positive cancers research[1].

IC50 & Target[1]

TrkA

 

体外研究
(In Vitro)

TRK-IN-33 (compound 20) (0.1-10 μM) 在 Ba/F3-LMNA-NTRK1WT 细胞 (表达野生型 TRKA 的细胞) 中，针对 TRKAG667C 耐药突变表现出优异的降解效率 (在 0.1 μM 浓度下降解率为 - 1.16%，在 1 μM 浓度下降解率为 69.30%，在 10 μM 浓度下降解率为 68.75%) 和抑制活性，其 IC50 为 23.8 nM[1]。
TRK-IN-33 (0.1-10 μM，处理 24 小时) 在 Ba/F3-LMNA-NTRK1G667C 细胞 (表达 G667C 突变型 TRKA 的细胞) 中，对 TRKAG667C 突变蛋白显示出良好的剂量依赖性降解[1]。
TRK-IN-33 (1 μM) 在 CD-1 小鼠、SD 大鼠或人源肝微粒体中表现出优越的药代动力学性质，其 T1/2 分别为 24.8、53.8 和 57.1 分钟；CLint 分别为 0.0683、0.0599 和 0.0230 mL/min/mg[1]。

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

TRK-IN-33 相关抗体:

Cell Viability Assay[1]

Cell Line: Ba/F3-LMNA-NTRK1G667C cells
Concentration: 0.1, 1 and 10 μM
Incubation Time: 24 h
Result: Exhibited > 90% maximal degradation, potentially overcoming on-target resistance in TRKA G667C resistant mutation.
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Mice[1] 1 mg/kg i.v. T1/2 0.249 h
Mice[1] 10 mg/kg p.o. T1/2 0.437 h
Mice[1] 1 mg/kg i.v. Tmax 0.083 h
Mice[1] 10 mg/kg p.o. Tmax 0.500 h
Mice[1] 1 mg/kg i.v. Cmax 590 ng/mL
Mice[1] 10 mg/kg p.o. Cmax 754 ng/mL
Mice[1] 1 mg/kg i.v. AUC0-t 231 ng·h/mL
Mice[1] 10 mg/kg p.o. AUC0-t 930 ng·h/mL
Mice[1] 1 mg/kg i.v. AUC0-∞ 232 ng·h/mL
Mice[1] 10 mg/kg p.o. AUC0-∞ 932 ng·h/mL
Mice[1] 1 mg/kg i.v. CL 442 mL/h/kg
Mice[1] 10 mg/kg p.o. CL 4313 mL/h/kg
Mice[1] 1 mg/kg i.v. MRT0-t 0.268 h
Mice[1] 10 mg/kg p.o. MRT0-t 0.903 h
Mice[1] 1 mg/kg i.v. MRT0-∞ 0.275 h
Mice[1] 10 mg/kg p.o. MRT0-∞ 0.911 h
Mice[1] 10 mg/kg p.o. F 40.2 %
体内研究
(In Vivo)

TRK-IN-33 (compound 20) (30 或 50 mg/kg，腹腔注射，每日两次，连续给药 28 天) 在 Ba/F3-LMNA-NTRK1G667C 小鼠移植瘤模型中能够克服由 G667C 突变驱动的 TRK 耐药并表现出良好的耐受性和安全性[1]。

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

Animal Model: Ba/F3-LMNA-NTRK1 sup>G667C cells (3 × 106) induced-female BALB/c nude mice (18-22 g, 4 weeks old)[1]
Dosage: 30 or 50 mg/kg
Administration: i.p., twice daily for 28 consecutive days
Result: Significantly inhibited tumor growth in a dose-dependent manner, with inhibition rates of 71.65 and 80.38% at 30 and 50 mg/kg, respectively.
Observed no statistically significant changes in body weight.
Revealed no apparent damage in major organs, including the heart, liver, spleen, lung, and kidney.
Revealed g a significant reduction of TRK fluorescence intensity.
Suppressed tumor cell proliferation and enhanced apoptosis in tumor tissues.
分子量

472.90

Formula

C22H22ClFN6O3
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-33 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-33Trk ReceptorApoptosisTropomyosin related kinase receptor TRKA G667C degradationinhibits tumor growthNTRK fusion?positive cancersTRKInhibitorinhibitorinhibit

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目录号：
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