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

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.

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DZX19

DZX19 Chemical Structure

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DZX19 Related Antibodies

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TrkA TrkB TrkC Trk

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Akt Akt1 Akt2 Akt3

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ERK ERK1 ERK2 ERK5 ERK8

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Description

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)

In Vitro

DZX19 (C02) (72 h) potently inhibits the proliferation of TRK fusion-positive and TRKA mutant-harboring cell lines, with greater efficacy than Entrectinib, and exhibits minimal off-target activity in TRK-negative A549 cells[1].
DZX19 (C02) (7.5-15 nM; 14 days) strongly suppresses the long-term colony-forming ability of TRK fusion-positive Km-12 cells more effectively than Entrectinib[1].
DZX19 (C02) (7.5-15 nM; 48 h) potently inhibits the migration of TRK fusion-positive Km-12 cells more effectively than Entrectinib[1].
DZX19 (C02) (7.5-30 nM; 24 h) dose-dependently induces G1 cell cycle arrest in TRK fusion-positive Km-12 cells, with stronger activity than Entrectinib[1].

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

DZX19 Related Antibodies

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..
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 /
In Vivo

DZX19 (20-40 mg/kg; p.o.; every day) dose-dependently inhibits tumor growth in a Km-12 colorectal cancer xenograft model[1].

MedChemExpress (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).
Molecular Weight

416.44

Formula

C20H18F2N4O2S
SMILES

NC(C1=C(SC=C1C2=CC(NCC3=CC(F)=CC(F)=C3)=CC=C2)NC(NC)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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DZX19 Related Classifications

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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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