DDR-TRK-1

Name: DDR-TRK-1
Brand: MedChemExpress
SKU: HY-100695
Rating: 4.5 (1 reviews)

Cat. No.: HY-100695 Purity: 98.90%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 1934246-19-1

Size	Price	Stock	Quantity
1 mg	USD 315	In-stock	Estimated Time of Arrival: December 31
5 mg		Get quote
10 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Discoidin Domain Receptor Isoform Specific Products:

View All Isoforms

DDR1 DDR2

Biological Activity
Protocol
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].

Cellular Effect

Cell Line	Type	Value	Description	References
Sf9	IC₅₀	> 10000 nM Compound: 6j	Inhibition of human full length recombinant His-tagged ABL1 expressed in baculovirus infected Sf9 insect cells using tyrosine 2 peptide as substrate preincubated for 1 hr measured after 2 hrs in presence of ATP by FRET-based Z'-Lyte assay Inhibition of human full length recombinant His-tagged ABL1 expressed in baculovirus infected Sf9 insect cells using tyrosine 2 peptide as substrate preincubated for 1 hr measured after 2 hrs in presence of ATP by FRET-based Z'-Lyte assay	[PMID: 27219676]
Sf9	IC₅₀	188 nM Compound: 6j	Inhibition of human recombinant GST-tagged DDR2 expressed in baculovirus infected Sf9 insect cells using fluorescein-poly GAT as substrate preincubated for 1 hr measured after 1 hr in presence of ATP by lance ultra kinase assay Inhibition of human recombinant GST-tagged DDR2 expressed in baculovirus infected Sf9 insect cells using fluorescein-poly GAT as substrate preincubated for 1 hr measured after 1 hr in presence of ATP by lance ultra kinase assay	[PMID: 27219676]
Sf9	IC₅₀	9.4 nM Compound: 6j	Inhibition of human recombinant GST-tagged DDR1 (440 to 876 residues) expressed in baculovirus infected Sf9 insect cells using fluorescein-poly GAT as substrate preincubated for 1 hr measured after 1 hr in presence of ATP by TR-FRET LanthaScreen assay Inhibition of human recombinant GST-tagged DDR1 (440 to 876 residues) expressed in baculovirus infected Sf9 insect cells using fluorescein-poly GAT as substrate preincubated for 1 hr measured after 1 hr in presence of ATP by TR-FRET LanthaScreen assay	[PMID: 27219676]

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 T_1/2 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 (K_d) value of 4.7 nM^[1].

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

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.

1934246-19-1

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
10 mM	0.2030 mL	1.0152 mL	2.0305 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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%

Select Batch:

Data Sheet (274 KB) SDS (252 KB)

COA (247 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

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	[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. [Content Brief]

Complete Stock Solution Preparation Table

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

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

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

DDR-TRK-1

Customer Review

DDR-TRK-1 Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Discoidin Domain Receptor Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

DDR-TRK-1 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

DDR-TRK-1 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report