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DDR-TRK-1

Catalog No. T10984 CAS 1934246-19-1

DDR-TRK-1 is a selective discoid domain receptor 1 (DDR1) inhibitor with IC50 value of 9.4 nM. DDR-TRK-1 also inhibits the TRK family.

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DDR-TRK-1, CAS 1934246-19-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 195.00
2 mg	In stock	$ 293.00
5 mg	In stock	$ 448.00
10 mg	In stock	$ 658.00
25 mg	In stock	$ 987.00
50 mg	In stock	$ 1,380.00
100 mg	In stock	$ 1,890.00
1 mL * 10 mM (in DMSO)	In stock	$ 539.00

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Purity: 99.86%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	DDR-TRK-1 is a selective discoid domain receptor 1 (DDR1) inhibitor with IC50 value of 9.4 nM. DDR-TRK-1 also inhibits the TRK family.
Targets&IC50	DDR1:9.4 nM
In vitro	DDR-TRK-1 is a promising candidate with an IC50 value of 9.4 nM relative to DDR1. DDR-TRK-1 also exhibited reasonable pharmacokinetic (PK) properties. At an oral dose of 20 mg/kg in rats, the oral bioavailability was 66.8%, and the T1/2 value was 1.25 h. However, the area under the concentration-time curve (AUC) value of DDR-TRK-1 in mice was significantly higher than that in rats, indicating that its absorption performance in mice was good. By determining the binding affinity of DDR1-IN-3 and DDR1 protein, the inhibitory effect of DDR1 on DDR1-IN-3 can be further verified. The results show that DDR-TRK-1 is closely bound to DDR1, and the binding constant (Kd) value is 4.7 nM[1].
In vivo	DDR-TRK-1 can prevent blm-induced pathological changes in a dose-dependent manner. These results agree with the expression levels of fibrosis markers in the lung tissue, including lysates, including fibronectin and α-smooth muscle actin (SMA). Further analysis also showed that the use of DDR-TRK-1 resulted in a dose-dependent inhibition of hydroxyproline content, a unique amino acid found in collagen. The above data indicate that DDR-TRK-1 has good therapeutic potential for blm-induced pulmonary fibrosis[1].

Molecular Weight	492.5
Formula	C26H23F3N6O
CAS No.	1934246-19-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (101.52 mM)

References and Literature

1. Zhen Wang, et al. Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors. J Med Chem. 2016 Jun 23; 59(12): 5911–5916.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

DDR-TRK-1 1934246-19-1 Tyrosine Kinase/Adaptors Discoidin Domain Receptor (DDR) DDRTRK1 DDR TRK 1 inhibitor inhibit

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