2. Protein Tyrosine Kinase/RTK
  3. Discoidin Domain Receptor
  4. DDR1-IN-1

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).

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

DDR1-IN-1 Chemical Structure

DDR1-IN-1 Chemical Structure

CAS No. : 1449685-96-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 120 In-stock
Solution
10 mM * 1 mL in DMSO USD 120 In-stock
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5 mg USD 99 In-stock
10 mg USD 154 In-stock
50 mg USD 290 In-stock
100 mg USD 450 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of DDR1-IN-1:

DDR1-IN-1 Related Antibodies

Top Publications Citing Use of Products

View All Discoidin Domain Receptor Isoform Specific Products:

View All Isoforms
DDR1 DDR2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].
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.

DDR1-IN-1 Related Antibodies
Molecular Weight

552.59

Formula

C30H31F3N4O3
CAS No.
Appearance

Solid

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
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 : 100 mg/mL (180.97 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 1.8097 mL 9.0483 mL 18.0966 mL
5 mM 0.3619 mL 1.8097 mL 3.6193 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: ≥ 2.5 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.

    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% (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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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: 98.20%

COA (247 KB) LCMS (150 KB)

Handling Instructions (2659 KB)
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 1.8097 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
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DDR1-IN-1 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:

DDR1-IN-11449685-96-4Discoidin Domain ReceptorInhibitorinhibitorinhibit

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