2. Protein Tyrosine Kinase/RTK
  3. Discoidin Domain Receptor
  4. DDR-TRK-1

DDR-TRK-1 is a selective Discoidin Domain Receptor 1 (DDR1) inhibitor, with an IC50 value of 9.4 nM. DDR-TRK-1 also inhibits TRK family.

For research use only. We do not sell to patients.

DDR-TRK-1 Chemical Structure

DDR-TRK-1 Chemical Structure

CAS No. : 1934246-19-1

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Based on 1 publication(s) in Google Scholar

DDR-TRK-1 Related Antibodies

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DDR1 DDR2

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  • Purity & Documentation

  • References

  • Customer Review

Description

DDR-TRK-1 is a selective Discoidin Domain Receptor 1 (DDR1) inhibitor, with an IC50 value of 9.4 nM. DDR-TRK-1 also inhibits TRK family.

IC50 & Target

IC50: 9.4 nM (DDR1)[1].
In Vitro

DDR-TRK-1 is a promising candidate, with an IC50 value of 9.4 nM against DDR1. DDR-TRK-1 also exhibits reasonable pharmacokinetic (PK) properties, with an oral bioavailability of 66.8% and a T1/2 value of 1.25 h at an oral dose of 20 mg/kg in rats. However, the area under concentration?time curve (AUC) value of DDR-TRK-1 in mice is obviously higher than that in rats, suggesting its good absorption property in mice. The DDR1 inhibition of DDR1-IN-3 is further validated by determining its binding affinity with the DDR1 protein. It is shown that DDR-TRK-1 bounds tightly to DDR1, with a binding constant (Kd) value of 4.7 nM[1].

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

DDR-TRK-1 Related Antibodies
In Vivo

DDR-TRK-1 prevents these BLM-induced pathological changes in a dose-dependent manner. These results agree with the expression levels of fibrotic markers in lung tissue lysates, including fibronectin and α-smooth muscle actin (SMA). Further analyses also reveal that the administration of DDR-TRK-1 cause a dose-dependent suppression in the content of hydroxyproline, a unique amino acid found in collagen. The above data collectively indicate the promising therapeutic potential of DDR-TRK-1 against the BLM-induced pulmonary fibrosis[1].

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

492.50

Formula

C26H23F3N6O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC(C(F)(F)F)=CC(N2C=C(C)N=C2)=C1)C(C=C3)=CC4=C3[C@@H](C)CN(C4)C5=CN=CN=C5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 40 mg/mL (81.22 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0305 mL 10.1523 mL 20.3046 mL
5 mM 0.4061 mL 2.0305 mL 4.0609 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.90%

COA (247 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

Panc-1 cells are plated at low density in media in the presence or absence of controls or the indicated concentration of DDR-TRK-1 (0.016, 0.0625, 0.25, 1 μM). Colony formation is evaluated after 1.5-2 weeks by fixing and staining with crystal violet. The effect of DDR1-IN-3 on cell migration is determined through a ‘scratch’ assay. Panc-1 cells are grown to confluence in a 6 well dish. A scratch is made using a p20 pipette tip and cell migration into the wound is determined at 12, 24, 48, 60, and 72 hrs. The effect of control compounds or DDR-TRK-1 at the indicated concentrations is determined at each time point[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
To induce pulmonary damage, 6- to 8-week-old sex- and age-matched wild type or slie mice (at least five animals per group) are intranasally dropped with bleomycin at 5mg/kg BW. The inhibitors (e.g., DDR-TRK-1) are dissolved in water at a concentration of 5 mg/mL and given to the mice orally by gavage twice a day. Hydroxyproline accounts for 13.4% of the total amino acids of collagen; thus its content can be used to reflect the severity of fibrosis. A commercial hydroxyproline kit is used. Briefly, fresh lung tissues are weighted and hydrolyzed to release hydroxyproline. After a series of chemical reactions, a pink color solution is formed and then subjected to measurement of absorbance at 560 nm. The hydroxyproline content of each sample is calculated by comparing with the standards[1].

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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0305 mL 10.1523 mL 20.3046 mL 50.7614 mL
5 mM 0.4061 mL 2.0305 mL 4.0609 mL 10.1523 mL
10 mM 0.2030 mL 1.0152 mL 2.0305 mL 5.0761 mL
15 mM 0.1354 mL 0.6768 mL 1.3536 mL 3.3841 mL
20 mM 0.1015 mL 0.5076 mL 1.0152 mL 2.5381 mL
25 mM 0.0812 mL 0.4061 mL 0.8122 mL 2.0305 mL
30 mM 0.0677 mL 0.3384 mL 0.6768 mL 1.6920 mL
40 mM 0.0508 mL 0.2538 mL 0.5076 mL 1.2690 mL
50 mM 0.0406 mL 0.2030 mL 0.4061 mL 1.0152 mL
60 mM 0.0338 mL 0.1692 mL 0.3384 mL 0.8460 mL
80 mM 0.0254 mL 0.1269 mL 0.2538 mL 0.6345 mL
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DDR-TRK-1 Related Classifications

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:

DDR-TRK-11934246-19-1Discoidin Domain ReceptorInhibitorinhibitorinhibit

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