2. Neuronal Signaling Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Stem Cell/Wnt MAPK/ERK Pathway Apoptosis
  3. Trk Receptor Akt ERK Apoptosis
  4. DZX19

DZX19 (Compound C02) 是一种具有口服活性的、选择性的 TRK 抑制剂，其 TRKA IC50 值为 1.32 nM，TRKB IC50 为 2.28 nM，TRKC IC50 为 4.05 nM。DZX19 可抑制野生型 TRKA、TRKA 突变体 (G595R、F589L、G667C)、野生型 TRKB 及野生型 TRKC 的激酶活性，并能抑制 TRKA 的磷酸化及其下游 AKT 和 ERK 信号通路。DZX19 可诱导凋亡 (Apoptosis)。DZX19 抑制结直肠癌异种移植小鼠模型中的肿瘤生长。DZX19 可用于结直肠癌的研究。

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DZX19

DZX19 Chemical Structure

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DZX19 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

查看 Akt 亚型特异性产品:

查看所有亚型
Akt Akt1 Akt2 Akt3

查看 ERK 亚型特异性产品:

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ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DZX19 (Compound C02) is an orally active, selective TRK inhibitor with a TRKA IC50 value of 1.32 nM, a TRKB IC50 of 2.28 nM, and a TRKC IC50 of 4.05 nM. DZX19 inhibits the kinase activities of wild-type TRKA, TRKA mutants (G595R, F589L, G667C), wild-type TRKB, and wild-type TRKC, and suppresses the phosphorylation of TRKA as well as its downstream AKT and ERK signaling pathways. DZX19 induces apoptosis. DZX19 inhibits tumor growth in a colorectal cancer xenograft mouse model. DZX19 is applicable for the research of colorectal cancer[1].

IC50 & Target[1]

TrkA

1.32 nM (IC50)

TrkB

2.28 nM (IC50)

TrkC

4.05 nM (IC50)

TRKAG595R

16.56 nM (IC50)

TRKAF589L

74.37 nM (IC50)

TRKAG667C

60.18 nM (IC50)

体外研究
(In Vitro)

DZX19 (72 h) 可强效抑制携带 TRKA 突变的细胞系增殖，其效果优于 Entrectinib (HY-12678)[1]。
DZX19 (7.5-15 nM；14 天) 对 Km-12 细胞的长期集落形成能力的抑制作用显著强于 Entrectinib[1]。
DZX19 (C02) (7.5-15 nM; 48 h) 可强效抑制 Km-12 细胞的迁移，其效果优于 Entrectinib[1]。
DZX19 (C02) (7.5-30 nM; 24 h) 可剂量依赖性地诱导 Km-12 细胞发生 G1 期细胞周期阻滞，且活性强于 Entrectinib[1]。

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

DZX19 相关抗体:

Cell Cycle Analysis[1]

Cell Line: Km-12
Concentration: 7.5-30 nM
Incubation Time: 24 h
Result: Induced a dose-dependent increase in the G1 phase ratio of Km-12 cells: 46.7% at 7.5 nM, 59.1% at 15 nM, and 66.2% at 30 nM.
Caused a corresponding decrease in the S phase ratio.
Showed more potent G1/S phase transition inhibition than Entrectinib at the same concentrations.

Apoptosis Analysis[1]

Cell Line: Km-12
Concentration: 7.5-30 nM
Incubation Time: 48 h
Result: Induced dose-dependent apoptosis in Km-12 cells, with apoptotic rates of 16.6% at 7.5 nM, 26.8% at 15 nM, and 36.6% at 30 nM (compared to 9.64% in the DMSO control).
Showed stronger pro-apoptotic activity than Entrectinib at the same concentrations.

Western Blot Analysis[1]

Cell Line: Km-12
Concentration: 7.5, 15, 30 nM
Incubation Time: 6 h
Result: Suppressed the phosphorylation of TRKA, ERK, and AKT in a dose-dependent manner..
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Tmax Cmax AUClast AUCinf CL MRT Vss F
Rat[1] 40 mg/kg p.o. 2.32 h 3.25 h 3437 ng/mL 21354 ng·h/mL 21377 ng·h/mL / 5.00 h / 172.9 %
Rat[1] 20 mg/kg p.o. 2.05 h 2.67 h 1250 ng/mL 7148 ng·h/mL 7705 ng·h/mL / 4.68 h / 124.6 %
Rat[1] 1 mg/kg i.v. 1.43 h 0.083 h 455 ng/mL 300 ng·h/mL 309 ng·h/mL 51.9 mL/min/kg 1.14 h 3551 mL/kg /
体内研究
(In Vivo)

DZX19 (20-40 mg/kg；口服；每日) 在 Km-12 结直肠癌异种移植模型中呈剂量依赖性抑制肿瘤生长[1]。

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

Animal Model: BALB/c-nu (female; subcutaneous xenograft model injected with 5×106 Km-12 cells)[1]
Dosage: 20 mg/kg; 40 mg/kg
Administration: p.o.; daily
Result: Achieved a tumor growth inhibition (TGI) rate of 60.2% at 20 mg/kg.
Achieved a tumor growth inhibition (TGI) rate of 82.7% at 40 mg/kg.
Caused no significant loss of body weight during the treatment period.
Showed no significant drug-induced toxicity via H&E staining of major organs (heart, liver, spleen, lungs, kidneys).
分子量

416.44

Formula

C20H18F2N4O2S
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

DZX19 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:

DZX19DZX 19DZX-19Trk ReceptorAktERKApoptosisTropomyosin related kinase receptor PKBProtein kinase BExtracellular signal regulated kinasesTRKCG667CPI3K/AKT signaling pathwaysTRKAcolorectal cancerF589LTPM3-NTRK1 fusion-positive cancer cellsTRKBMEK/ERK signaling pathwaysG595RInhibitorinhibitorinhibit

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