DDR1-IN-1
Based on 6 publication(s) in Google Scholar
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.
- Purity: 98.0%
- CAS No.: 1449685-96-4
- Formula: C30H31F3N4O3
- Molecular Weight:552.59
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) DDR1-IN-1
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
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WB
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WB
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Cell Imaging/Staining
Biological Activity
IC50: 105 nM (DDR1)[1].
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Cell Line
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Type | Value | Description | References |
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| Sf9 | IC50 |
105 nM
Compound: 18, DDR1-IN-1
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Inhibition of human DDR1 kinase domain (601 to 913 residues) expressed in Sf9 cells by enzymatic kinase assay
Inhibition of human DDR1 kinase domain (601 to 913 residues) expressed in Sf9 cells by enzymatic kinase assay
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[PMID: 25569119] |
| U2OS | EC50 |
86 nM
Compound: 1; DDR1-IN-1
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Antiproliferative activity against human U2OS cells harboring DDR1-IN-1 assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Antiproliferative activity against human U2OS cells harboring DDR1-IN-1 assessed as reduction in cell viability incubated for 24 hrs by MTT assay
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[PMID: 38452728] |
| U2OS | IC50 |
86 nM
Compound: 18, DDR1-IN-1
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Inhibition of human DDR1 in doxycycline-stimulated human U2OS cells assessed as inhibition of collagen-1-induced autophosphorylation incubated for 1 hr
Inhibition of human DDR1 in doxycycline-stimulated human U2OS cells assessed as inhibition of collagen-1-induced autophosphorylation incubated for 1 hr
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[PMID: 25569119] |
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.
Chemical Information
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CAS No. 1449685-96-4
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Appearance Solid
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Molecular Weight 552.59
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Formula C30H31F3N4O3
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Color Light yellow to yellow
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Cell Death Differ
Dual targeting of chemoresistance and ferroptosis in gastric cancer: DDR1/VEGFR2 inhibitor K-13 synergizes with docetaxel from preclinical models to phase Ib/II clinical trial. [Abstract]2026 May 13. PMID: 42128929 -
Cell Death Discov
Discoidin domain receptor inhibitor DDR1-IN-1 induces autophagy and necroptotic cell death in malignant peripheral nerve sheath tumor. [Abstract]2025 Mar 1;11(1):83. PMID: 40025071
DDR1-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Mar 1;11(1):83. [Abstract]
To identify potential inhibitors that perform anti-MPNST activity, we introduced 3 inhibitors and 1 clinical-used anti-cancer drug to an MPNST cell line, S462. 0-100 μM DDR1-IN-1, Doxorubicin, JQ-1 and SHP099 were introduced to cells for 48 hours. Cell viability was evaluated through the MTT assay, and the IC25, IC50, and IC75 were calculated.
DDR1-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Mar 1;11(1):83. [Abstract]
Images of cells treated with indicated doses of Doxorubicin and DDR1-IN-1 for 24 hours were shown.
DDR1-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Mar 1;11(1):83. [Abstract]
The total protein lysates of S462 treated with 0-10 μM DDR1-IN-1 for 24 hours were extracted. Western blotting was performed to reveal the expression levels of various cell death-related proteins that participated in the autophagy or apoptosis pathway. The red arrowheads point out the cleaved PARP.
DDR1-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Mar 1;11(1):83. [Abstract]
Autophagy inhibitor, 3-MA (5 mM), was co-treated separately with 10 μM DDR1-IN-1 to S462 cells for 24 hours. Total protein was extracted and the cell death-related markers were demonstrated through western blotting. The cleaved-Caspase3 is pointed out by the red arrow.
DDR1-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Mar 1;11(1):83. [Abstract]
The fluorescent images represent the S462 cells under AO assay in response to 0-15 μM DDR1-IN-1 treatment for 24 hours. Green fluorescent represents the cytoplasm and nucleus; red fluorescent indicates the acidic vacuoles and the white arrows point to the cells undergoing autophagy. Transcriptomic data are also presented.
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Int J Biol Macromol
Human type III collagen-derived biomaterial with high antitumor activity inhibits breast cancer cell autophagy, proliferation, and migration through DDR1. [Abstract]2023 Jul 15:243:125130. PMID: 37263336 -
Cancers
Discoidin Domain Receptor-1 (DDR1) is Involved in Angiolymphatic Invasion in Oral Cancer. [Abstract]2020 Mar 31;12(4):841. PMID: 32244515 -
Exp Ther Med
3D culture enhances chemoresistance of ALL Jurkat cell line by increasing DDR1 expression. [Abstract]2019 Mar;17(3):1593-1600. PMID: 30783426
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (272 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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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 |
DDR1-IN-1 Related Classifications
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