Home Protein Tyrosine Kinase Trk receptor inhibitor CH7057288 For research use only.

CH7057288

CH7057288 is a potent and selective TRK inhibitor with IC50 values of 1.1 nM, 7.8 nM and 5.1 nM for TRKA, TRKB, and TRKC respectively.

CH7057288 Chemical Structure

CH7057288 Chemical Structure

CAS: 2095616-82-1

Purity & Quality Control

Batch: S878801 DMSO] 100 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.50%
99.50

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Signaling Pathway

Trk receptor Signaling Pathways

Trk receptor Signaling Pathway

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Biological Activity

Description CH7057288 is a potent and selective TRK inhibitor with IC50 values of 1.1 nM, 7.8 nM and 5.1 nM for TRKA, TRKB, and TRKC respectively.
Targets
TrkA [1]
(Cell-free assay)		 TrkC [1]
(Cell-free assay)		 TrkB [1]
(Cell-free assay)
1.1 nM 5.1 nM 7.8 nM
In vitro
In vitro

CH7057288 shows selective inhibitory activity against TRKA, TRKB, and TRKC in cell-free kinase assays and suppresses proliferation of TRK fusion-positive cell lines, but not that of TRK-negative cell lines. CH7057288 suppresses mitogen-activated protein kinase (MAPK) and E2F pathways as downstream signaling of TRK fusion[1].
Cell Research Cell lines The NSCLC cell line CUTO-3, CRC cell line KM12-Luc, and acute myeloid leukemia cell line MO-91 harbor MPRIP-NTRK1, TPM3-NTRK1, and ETV6-NTRK3, respectively
Concentrations 0.01, 0.1 and 1 μM
Incubation Time 2 h
Method

TRK fusion-positive cancer cell lines CUTO-3, KM12-Luc, and MO-91 are treated with the indicated concentrations of CH7057288 for 2 hours. The cells are lysed and analyzed by western blotting.
In Vivo
In vivo

Strong in vivo tumor growth inhibition is observed in subcutaneously implanted xenograft tumor models of TRK fusion-positive cells. Furthermore, in an intracranial implantation model mimicking brain metastasis, CH7057288 significantly induces tumor regression and improves event-free survival. CH7057288 induces potent tumor growth inhibition against all three models, with remarkable tumor regression in CUTO-3 and MO-91. CH7057288 exhibits dose-dependent exposure. Because of relatively short terminal half-life (3 to 5 hours), the plasma concentration 24 hours after dose dropped to approximately a few tenths to a hundredth of Tmax[1].

Chemical Information & Solubility

Molecular Weight 569.67 Formula

C32H31N3O5S
CAS No. 2095616-82-1 SDF --
Smiles CC1=CC(=CC(=N1)C#CC2=CC3=C(C=C2)C4=C(O3)C(C5=C(C4=O)C=CC(=C5)NS(=O)(=O)C)(C)C)C(=O)NC(C)(C)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (175.54 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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