Art. -Nr.: HY-U00444

7rh

(Synonyms: DDR1-IN-2)

6 Cited Publications

Kundenbewertung

Based on 6 publication(s) in Google Scholar

7rh (DDR1-IN-2) is a potent inhibitor of discoidin domain receptor 1 (DDR1), with an IC₅₀ of 13.1 nM, and also less potently inhibits DDR2, with an IC₅₀ of 203 nM. 7rh is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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Reinheit: 99.31%
CAS. Nr.: 1429617-90-2
Formel: C₃₀H₂₉F₃N₆O
Molecular Weight:546.59

Speicherung:

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

7rh Chemical Structure

CAS. Nr.: 1429617-90-2

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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
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 13.1 nM (DDR1), 203 nM (DDR2), 414 nM (Bcr-Abl), 2500 nM (c-Kit)^[1]

Alle Discoidin Domain Receptor Isoform-spezifische Produkte anzeigen :

DDR1
DDR2

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	2.74 μM Compound: 7rh	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 23521020]
HCT-116	IC₅₀	1.13 μM Compound: 7rh	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 23521020]
K562	IC₅₀	0.038 μM Compound: 7rh	Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay	[PMID: 23521020]
MCF7	IC₅₀	2.15 μM Compound: 7rh	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 23521020]
MDA-MB-435S	IC₅₀	2.22 μM Compound: 7rh	Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay	[PMID: 23521020]
NCI-H23	IC₅₀	0.56 μM Compound: 7rh	Cytotoxicity against human NCI-H23 cell assessed as inhibition of colony formation after 10 days by clonogenic assay Cytotoxicity against human NCI-H23 cell assessed as inhibition of colony formation after 10 days by clonogenic assay	[PMID: 23521020]
NCI-H23	IC₅₀	2.08 μM Compound: 7rh	Antiproliferative activity against human NCI-H23 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H23 cells after 72 hrs by MTT assay	[PMID: 23521020]
NCI-H460	IC₅₀	2.98 μM Compound: 7rh	Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay	[PMID: 23521020]
T47D	IC₅₀	1.88 μM Compound: 7rh	Antiproliferative activity against human T47D cells after 72 hrs by MTT assay Antiproliferative activity against human T47D cells after 72 hrs by MTT assay	[PMID: 23521020]

In Vitro

7rh (compound 1) is a potent inhibitor of DDR1, with an IC₅₀ of 13.1 nM, and less potently inhibits DDR2, with an IC₅₀ of 203 nM. 7rh also shows inhibitory activities against Bcr-Abl and c-Kit, with IC₅₀s of 414 and 2500 nM, respectively^[1].

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

Chemical Information

CAS. Nr. 1429617-90-2
Appearance Solid
Molecular Weight 546.59
Formel C₃₀H₂₉F₃N₆O
Color White to light yellow
SMILES

O=C(NC1=CC(C(F)(F)F)=CC(CN2CCN(C)CC2)=C1)C3=CC=C(CC)C(C#CC4=CN5C(N=C4)=CC=N5)=C3
Synonyms

DDR1-IN-2
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)

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Journal Impact Factor

Cell Death Differ

Collagen I-DDR1 signaling promotes hepatocellular carcinoma cell stemness via Hippo signaling repression. [Abstract]

2023 Jul;30(7):1648-1665. PMID: 37117273
Cell Rep Med

Loss of p53 and SMAD4 induces adenosquamous subtype pancreatic cancer in the absence of an oncogenic KRAS mutation. [Abstract]

2024 Aug 29:101711. PMID: 39232498
NPJ Precis Oncol

DDR1 is identified as an immunotherapy target for microsatellite stable colon cancer by CRISPR screening. [Abstract]

2024 Nov 7;8(1):253. PMID: 39511298
J Transl Med

Inhibition of DDR1 potentiates carbon ion radiotherapy by promoting ferroptosis and immunogenic death in head and neck squamous cell carcinoma. [Abstract]

2025 Sep 24;23(1):1011. PMID: 40993737
Oncogene

DDR1 promotes hepatocellular carcinoma metastasis through recruiting PSD4 to ARF6. [Abstract]

2022 Mar;41(12):1821-1834. PMID: 35140331
Research Square Print

2022 Jun.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 62.5 mg/mL (114.35 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

1.8295 mL

9.1476 mL

18.2952 mL

5 mM

0.3659 mL

1.8295 mL

3.6590 mL

10 mM

0.1830 mL

0.9148 mL

1.8295 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: ≥ 2.08 mg/mL (3.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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

Protokoll

Kinase Assay^[1]

The effects of compounds (including DDR1-IN-2) on the kinases DDR1 and DDR2 are assessed by using a LanthaScreen Eu kinase activity assay technology. Kinase reactions are performed in a 10 µL solution in low-volume 384-well plates. The kinase reaction buffer consists of 50 mM HEPES pH 7.5, 0.01% BRIJ-35, 10 mM MgCl₂, and 1 mM EGTA; the concentration of Fluorescein-Poly GAT substrate in the assay is 100 nM. Kinase reactions are initiated by the addition of 100 nM ATP in the presence of serially diluted compounds (DDR1-IN-2). The reactions are allowed to proceed for 1 h at room temperature before a 10 µL preparation of EDTA (20 mM) and Eu-labeled antibody (4 nM) in TR-FRET dilution buffer are added. The final concentration of antibody in the assay well is 2 nM, and the final concentration of EDTA is 10 mM. The plate is allowed to incubate at room temperature for one more hour before the TR-FRET emission ratios of 665 nm/340 nm are acquired on a multilabel reader. Data analysis and curve fitting are performed using GraphPad Prism4 software^[1].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Wang Z, et al. Tetrahydroisoquinoline-7-carboxamide Derivatives as New Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors. ACS Med Chem Lett. 2017 Feb 9;8(3):327-332. [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	1.8295 mL	9.1476 mL	18.2952 mL	45.7381 mL
	5 mM	0.3659 mL	1.8295 mL	3.6590 mL	9.1476 mL
	10 mM	0.1830 mL	0.9148 mL	1.8295 mL	4.5738 mL
	15 mM	0.1220 mL	0.6098 mL	1.2197 mL	3.0492 mL
	20 mM	0.0915 mL	0.4574 mL	0.9148 mL	2.2869 mL
	25 mM	0.0732 mL	0.3659 mL	0.7318 mL	1.8295 mL
	30 mM	0.0610 mL	0.3049 mL	0.6098 mL	1.5246 mL
	40 mM	0.0457 mL	0.2287 mL	0.4574 mL	1.1435 mL
	50 mM	0.0366 mL	0.1830 mL	0.3659 mL	0.9148 mL
	60 mM	0.0305 mL	0.1525 mL	0.3049 mL	0.7623 mL
	80 mM	0.0229 mL	0.1143 mL	0.2287 mL	0.5717 mL
	100 mM	0.0183 mL	0.0915 mL	0.1830 mL	0.4574 mL

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7rh

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound 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

Alkyne Compound Library

Publications Citing Use of MedChemExpress (MCE) 7rh

Alle Discoidin Domain Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

7rh

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound 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

Alkyne Compound Library

Publications Citing Use of MedChemExpress (MCE) 7rh

Alle Discoidin Domain Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

7rh Related Classifications

HY-U00444 Related Classifications