2. Protein Tyrosine Kinase/RTK
  3. Discoidin Domain Receptor
  4. 7rh

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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7rh Chemical Structure

7rh Chemical Structure

CAS No. : 1429617-90-2

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 156 In-stock
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5 mg USD 130 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

7rh Related Antibodies

Top Publications Citing Use of Products

View All Discoidin Domain Receptor Isoform Specific Products:

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DDR1 DDR2

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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.

IC50 & Target

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

7rh Related Antibodies
Molecular Weight

546.59

Formula

C30H29F3N6O
CAS No.
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
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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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)

g

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%

COA (245 KB) LCMS (271 KB)

Handling Instructions (2659 KB)
References
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

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.

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 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:

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

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