1. Protein Tyrosine Kinase/RTK
  2. Discoidin Domain Receptor
  3. DDR Inhibitor

DDR Inhibitor is a potent discoidin domain receptor (DDR) inhibitor, with an IC50 of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM.

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

DDR Inhibitor Chemical Structure

DDR Inhibitor Chemical Structure

CAS No. : 1644069-80-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 550 In-stock
Solution
10 mM * 1 mL in DMSO USD 550 In-stock
Solid
1 mg USD 250 In-stock
5 mg USD 500 In-stock
10 mg USD 800 In-stock
25 mg USD 1600 In-stock
50 mg USD 2560 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

DDR Inhibitor is a potent discoidin domain receptor (DDR) inhibitor, with an IC50 of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM.

IC50 & Target

IC50: 3.3 nM (DDR2)[1]
IC53: 1.5 nM (DDR1)[1]

In Vitro

DDR Inhibitor (Example 6) is a potent DDR inhibitor, with an IC50 of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM[1].

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

Molecular Weight

417.44

Formula

C23H20FN5O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CN=C2C=CC=CN21)NC3=CC(CNC(NC4=CC=CC(F)=C4)=O)=CC=C3C

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 : 65 mg/mL (155.71 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 2.3956 mL 11.9778 mL 23.9555 mL
5 mM 0.4791 mL 2.3956 mL 4.7911 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: ≥ 2.17 mg/mL (5.20 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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: ≥ 2.17 mg/mL (5.20 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.17 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 (21.7 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
References
Kinase Assay
[1]

Europium Kinase binding assay is used. Compounds (DDR Inhibitor, etc.) are incubated with 0.5 nM DDR1 or 0.25 nM DDR2 for 1 hour at room temperature in low volume black 384 well assay plates containing 5 nM or 10 nM Kinase Tracer 178 respectively and 2 nM Europium labelled anti-GST antibody in assay buffer (50 mM HEPES pH 7.5, 10 mM MgCl2, 1 mM EGTA and 0.01 % BRIJ35). The ratio of fluorescence emission 665 nm/615 nm after excitation at 340 nm is obtained. IC50 values are determined from dose-response plots using nonlinear least-squares analysis[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 2.3956 mL 11.9778 mL 23.9555 mL 59.8888 mL
5 mM 0.4791 mL 2.3956 mL 4.7911 mL 11.9778 mL
10 mM 0.2396 mL 1.1978 mL 2.3956 mL 5.9889 mL
15 mM 0.1597 mL 0.7985 mL 1.5970 mL 3.9926 mL
20 mM 0.1198 mL 0.5989 mL 1.1978 mL 2.9944 mL
25 mM 0.0958 mL 0.4791 mL 0.9582 mL 2.3956 mL
30 mM 0.0799 mL 0.3993 mL 0.7985 mL 1.9963 mL
40 mM 0.0599 mL 0.2994 mL 0.5989 mL 1.4972 mL
50 mM 0.0479 mL 0.2396 mL 0.4791 mL 1.1978 mL
60 mM 0.0399 mL 0.1996 mL 0.3993 mL 0.9981 mL
80 mM 0.0299 mL 0.1497 mL 0.2994 mL 0.7486 mL
100 mM 0.0240 mL 0.1198 mL 0.2396 mL 0.5989 mL
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DDR Inhibitor 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.

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DDR Inhibitor
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