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DDR-TRK-1

🥰Excellent
Catalog No. T10984Cas No. 1934246-19-1

DDR-TRK-1, a selective discoid domain receptor 1 (DDR1) inhibitor, exhibits an IC50 value of 9.4 nM and also inhibits the TRK family.

DDR-TRK-1

DDR-TRK-1

🥰Excellent
Purity: 99.86%
Catalog No. T10984Cas No. 1934246-19-1
DDR-TRK-1, a selective discoid domain receptor 1 (DDR1) inhibitor, exhibits an IC50 value of 9.4 nM and also inhibits the TRK family.
Pack SizePriceAvailabilityQuantity
1 mg$117In Stock
2 mg$175In Stock
5 mg$268In Stock
10 mg$394In Stock
25 mg$592In Stock
50 mg$828In Stock
100 mgInquiryIn Stock
1 mL x 10 mM (in DMSO)$323In Stock
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Purity:99.86%
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Product Introduction

Bioactivity
Description
DDR-TRK-1, a selective discoid domain receptor 1 (DDR1) inhibitor, exhibits an IC50 value of 9.4 nM and 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. It exhibited reasonable pharmacokinetic (PK) properties, with an oral bioavailability of 66.8% and a T1/2 value of 1.25 h at a 20 mg/kg oral dose in rats. The area under the concentration-time curve (AUC) value in mice was significantly higher than in rats, indicating good absorption performance in mice. Binding affinity studies of DDR1-IN-3 and DDR1 protein further verified DDR-TRK-1's inhibitory effect on DDR1, showing a binding constant (Kd) value of 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].
Chemical Properties
Molecular Weight492.5
FormulaC26H23F3N6O
Cas No.1934246-19-1
SmilesC[C@@H]1C=2C(CN(C1)C=3C=NC=NC3)=CC(C(NC4=CC(=CC(C(F)(F)F)=C4)N5C=NC(C)=C5)=O)=CC2
Relative Density.1.37 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (101.52 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0305 mL10.1523 mL20.3046 mL101.5228 mL
5 mM0.4061 mL2.0305 mL4.0609 mL20.3046 mL
10 mM0.2030 mL1.0152 mL2.0305 mL10.1523 mL
20 mM0.1015 mL0.5076 mL1.0152 mL5.0761 mL
50 mM0.0406 mL0.2030 mL0.4061 mL2.0305 mL
100 mM0.0203 mL0.1015 mL0.2030 mL1.0152 mL

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