Art. -Nr.: HY-13979

DDR1-IN-1

6 Cited Publications

Kundenbewertung

Based on 6 publication(s) in Google Scholar

DDR1-IN-1 is a potent and selective DDR1 receptor tyrosine kinase inhibitor with an IC₅₀ of 105 nM; 4-fold less potent for DDR2 (IC₅₀ = 413 nM).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 98.0%
CAS. Nr.: 1449685-96-4
Formel: C₃₀H₃₁F₃N₄O₃
Molecular Weight:552.59

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

DDR1-IN-1 Chemical Structure

CAS. Nr.: 1449685-96-4

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (6)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

DDR1-IN-1 is a potent and selective DDR1 receptor tyrosine kinase inhibitor with an IC₅₀ of 105 nM; 4-fold less potent for DDR2 (IC₅₀ = 413 nM)^[1].

IC₅₀ & Target

IC50: 105 nM (DDR1)^[1].

Alle Discoidin Domain Receptor Isoform-spezifische Produkte anzeigen :

DDR1
DDR2

Cellular Effect

Cell Line	Type	Value	Description	References
Sf9	IC₅₀	105 nM Compound: 18, DDR1-IN-1	Inhibition of human DDR1 kinase domain (601 to 913 residues) expressed in Sf9 cells by enzymatic kinase assay Inhibition of human DDR1 kinase domain (601 to 913 residues) expressed in Sf9 cells by enzymatic kinase assay	[PMID: 25569119]
U2OS	EC₅₀	86 nM Compound: 1; DDR1-IN-1	Antiproliferative activity against human U2OS cells harboring DDR1-IN-1 assessed as reduction in cell viability incubated for 24 hrs by MTT assay Antiproliferative activity against human U2OS cells harboring DDR1-IN-1 assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 38452728]
U2OS	IC₅₀	86 nM Compound: 18, DDR1-IN-1	Inhibition of human DDR1 in doxycycline-stimulated human U2OS cells assessed as inhibition of collagen-1-induced autophosphorylation incubated for 1 hr Inhibition of human DDR1 in doxycycline-stimulated human U2OS cells assessed as inhibition of collagen-1-induced autophosphorylation incubated for 1 hr	[PMID: 25569119]

In Vitro

DDR1-IN-1 effectively blocks collagen-induced DDR1 pY513 autophosphorylation in U2OS cells (EC₅₀ = 86.76 nM) with excellent selectivity over a panel of >380 kinases. DDR1-IN-1 inhibits DDR2-mediated MT1-MMP activation in human rheumatoid synovial fibroblasts (RASF) upon collagen stimulation (IC₅₀ < 2.5 μM) and enhances PI3K/mTOR inhibitor GSK2126458 antiproliferation efficacy in SNU-1040 colorectal cancer culture^[1].

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

Chemical Information

CAS. Nr. 1449685-96-4
Appearance Solid
Molecular Weight 552.59
Formel C₃₀H₃₁F₃N₄O₃
Color Light yellow to yellow
SMILES

O=C(NC1=CC=C(C)C(OC2=CC3=C(NC(C3)=O)C=C2)=C1)C4=CC=C(CN5CCN(CC)CC5)C(C(F)(F)F)=C4
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (6)

All Cell Proliferation/Viability AssayCell Imaging/StainingWB

Sort by:

Journal Impact Factor

Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Cell Death Differ

Dual targeting of chemoresistance and ferroptosis in gastric cancer: DDR1/VEGFR2 inhibitor K-13 synergizes with docetaxel from preclinical models to phase Ib/II clinical trial. [Abstract]

2026 May 13. PMID: 42128929
Cell Death Discov

Discoidin domain receptor inhibitor DDR1-IN-1 induces autophagy and necroptotic cell death in malignant peripheral nerve sheath tumor. [Abstract]

2025 Mar 1;11(1):83. PMID: 40025071

DDR1-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Mar 1;11(1):83. [Abstract]

To identify potential inhibitors that perform anti-MPNST activity, we introduced 3 inhibitors and 1 clinical-used anti-cancer drug to an MPNST cell line, S462. 0-100 μM DDR1-IN-1, Doxorubicin, JQ-1 and SHP099 were introduced to cells for 48 hours. Cell viability was evaluated through the MTT assay, and the IC₂₅, IC₅₀, and IC₇₅ were calculated.

DDR1-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Mar 1;11(1):83. [Abstract]

Images of cells treated with indicated doses of Doxorubicin and DDR1-IN-1 for 24 hours were shown.

DDR1-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Mar 1;11(1):83. [Abstract]

The total protein lysates of S462 treated with 0-10 μM DDR1-IN-1 for 24 hours were extracted. Western blotting was performed to reveal the expression levels of various cell death-related proteins that participated in the autophagy or apoptosis pathway. The red arrowheads point out the cleaved PARP.

DDR1-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Mar 1;11(1):83. [Abstract]

Autophagy inhibitor, 3-MA (5 mM), was co-treated separately with 10 μM DDR1-IN-1 to S462 cells for 24 hours. Total protein was extracted and the cell death-related markers were demonstrated through western blotting. The cleaved-Caspase3 is pointed out by the red arrow.

DDR1-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Mar 1;11(1):83. [Abstract]

The fluorescent images represent the S462 cells under AO assay in response to 0-15 μM DDR1-IN-1 treatment for 24 hours. Green fluorescent represents the cytoplasm and nucleus; red fluorescent indicates the acidic vacuoles and the white arrows point to the cells undergoing autophagy. Transcriptomic data are also presented.
Int J Biol Macromol

Human type III collagen-derived biomaterial with high antitumor activity inhibits breast cancer cell autophagy, proliferation, and migration through DDR1. [Abstract]

2023 Jul 15:243:125130. PMID: 37263336
Cancers

Discoidin Domain Receptor-1 (DDR1) is Involved in Angiolymphatic Invasion in Oral Cancer. [Abstract]

2020 Mar 31;12(4):841. PMID: 32244515
Exp Ther Med

3D culture enhances chemoresistance of ALL Jurkat cell line by increasing DDR1 expression. [Abstract]

2019 Mar;17(3):1593-1600. PMID: 30783426

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (180.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8097 mL

9.0483 mL

18.0966 mL

5 mM

0.3619 mL

1.8097 mL

3.6193 mL

10 mM

0.1810 mL

0.9048 mL

1.8097 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (4.52 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Kim HG, et al. Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. ACS Chem Biol. 2013 Oct 18;8(10):2145-50. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8097 mL	9.0483 mL	18.0966 mL	45.2415 mL
	5 mM	0.3619 mL	1.8097 mL	3.6193 mL	9.0483 mL
	10 mM	0.1810 mL	0.9048 mL	1.8097 mL	4.5241 mL
	15 mM	0.1206 mL	0.6032 mL	1.2064 mL	3.0161 mL
	20 mM	0.0905 mL	0.4524 mL	0.9048 mL	2.2621 mL
	25 mM	0.0724 mL	0.3619 mL	0.7239 mL	1.8097 mL
	30 mM	0.0603 mL	0.3016 mL	0.6032 mL	1.5080 mL
	40 mM	0.0452 mL	0.2262 mL	0.4524 mL	1.1310 mL
	50 mM	0.0362 mL	0.1810 mL	0.3619 mL	0.9048 mL
	60 mM	0.0302 mL	0.1508 mL	0.3016 mL	0.7540 mL
	80 mM	0.0226 mL	0.1131 mL	0.2262 mL	0.5655 mL
	100 mM	0.0181 mL	0.0905 mL	0.1810 mL	0.4524 mL

Keywords

DDR1-IN-1

6 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

DDR1-IN-1

Chemical Probe Library

Targeted Diversity Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Publications Citing Use of MedChemExpress (MCE) DDR1-IN-1

Alle Discoidin Domain Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

DDR1-IN-1

Chemical Probe Library

Targeted Diversity Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Publications Citing Use of MedChemExpress (MCE) DDR1-IN-1

Alle Discoidin Domain Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

DDR1-IN-1 Related Classifications

HY-13979 Related Classifications