DDR1-IN-1 dihydrochloride
Based on 6 publication(s) in Google Scholar
DDR1-IN-1 dihydrochloride 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: 98.92%
- CAS No.: 1780303-76-5
- Formula: C30H33Cl2F3N4O3
- Molecular Weight:625.51
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
Publications Citing Use of MedChemExpress (MCE) DDR1-IN-1 dihydrochloride
More
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
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DDR1 105 nM (IC50) |
DDR2 413 nM (IC50) |
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. 1780303-76-5
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Appearance Solid
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Molecular Weight 625.51
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Formula C30H33Cl2F3N4O3
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Color Light yellow to yellow
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SMILES
CC1=C(C=C(C=C1)NC(C2=CC=C(C(C(F)(F)F)=C2)CN3CCN(CC3)CC)=O)OC4=CC(C5)=C(C=C4)NC5=O.Cl.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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
H2O : 100 mg/mL (159.87 mM; ultrasonic and warming and heat to 60°C)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| H2O | 1 mM | 1.5987 mL | 7.9935 mL | 15.9870 mL | 39.9674 mL |
| 5 mM | 0.3197 mL | 1.5987 mL | 3.1974 mL | 7.9935 mL | |
| 10 mM | 0.1599 mL | 0.7993 mL | 1.5987 mL | 3.9967 mL | |
| 15 mM | 0.1066 mL | 0.5329 mL | 1.0658 mL | 2.6645 mL | |
| 20 mM | 0.0799 mL | 0.3997 mL | 0.7993 mL | 1.9984 mL | |
| 25 mM | 0.0639 mL | 0.3197 mL | 0.6395 mL | 1.5987 mL | |
| 30 mM | 0.0533 mL | 0.2664 mL | 0.5329 mL | 1.3322 mL | |
| 40 mM | 0.0400 mL | 0.1998 mL | 0.3997 mL | 0.9992 mL | |
| 50 mM | 0.0320 mL | 0.1599 mL | 0.3197 mL | 0.7993 mL | |
| 60 mM | 0.0266 mL | 0.1332 mL | 0.2664 mL | 0.6661 mL | |
| 80 mM | 0.0200 mL | 0.0999 mL | 0.1998 mL | 0.4996 mL | |
| 100 mM | 0.0160 mL | 0.0799 mL | 0.1599 mL | 0.3997 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
DDR1-IN-1 dihydrochloride Related Classifications
HY-13979A Related Classifications
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