7rh (Synonyms: DDR1-IN-2)

Name: 7rh
Brand: MedChemExpress
SKU: HY-U00444
Rating: 5.0 (4 reviews)

Cat. No.: HY-U00444 Purity: 99.54%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

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

7rh Chemical Structure

CAS No. : 1429617-90-2

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 156	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 156	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 130	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 210	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 438	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 668	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 978	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 4 publication(s) in Google Scholar

4 Publications Citing Use of MCE 7rh

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DDR1 DDR2

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

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

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.

Molecular Weight

546.59

Formula

C₃₀H₂₉F₃N₆O

CAS No.

1429617-90-2

Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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.

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:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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

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.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.54%

Select Batch:

Data Sheet (272 KB) SDS (252 KB)

COA (245 KB) LCMS (271 KB)

Handling Instructions (2659 KB)

References

[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]

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].

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

References

[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]

Complete Stock Solution Preparation Table

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

7rh Related Classifications

Inflammation/Immunology

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:

7rh1429617-90-2DDR1-IN-2Discoidin Domain ReceptorInhibitorinhibitorinhibit

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7rh (Synonyms: DDR1-IN-2)

Customer Review

7rh Related Antibodies

4 Publications Citing Use of MCE 7rh

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

7rh Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

7rh Related Classifications

Keywords:

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