7rh
Based on 6 publication(s) in Google Scholar
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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.31%
- CAS 番号: 1429617-90-2
- 分子式: C30H29F3N6O
- 分子量:546.59
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 7rh
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生物活性
IC50: 13.1 nM (DDR1), 203 nM (DDR2), 414 nM (Bcr-Abl), 2500 nM (c-Kit)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
2.74 μM
Compound: 7rh
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Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
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[PMID: 23521020] |
| HCT-116 | IC50 |
1.13 μM
Compound: 7rh
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Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
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[PMID: 23521020] |
| K562 | IC50 |
0.038 μM
Compound: 7rh
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Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay
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[PMID: 23521020] |
| MCF7 | IC50 |
2.15 μM
Compound: 7rh
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Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
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[PMID: 23521020] |
| MDA-MB-435S | IC50 |
2.22 μM
Compound: 7rh
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Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay
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[PMID: 23521020] |
| NCI-H23 | IC50 |
0.56 μM
Compound: 7rh
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Cytotoxicity against human NCI-H23 cell assessed as inhibition of colony formation after 10 days by clonogenic assay
Cytotoxicity against human NCI-H23 cell assessed as inhibition of colony formation after 10 days by clonogenic assay
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[PMID: 23521020] |
| NCI-H23 | IC50 |
2.08 μM
Compound: 7rh
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Antiproliferative activity against human NCI-H23 cells after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H23 cells after 72 hrs by MTT assay
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[PMID: 23521020] |
| NCI-H460 | IC50 |
2.98 μM
Compound: 7rh
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Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay
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[PMID: 23521020] |
| T47D | IC50 |
1.88 μM
Compound: 7rh
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Antiproliferative activity against human T47D cells after 72 hrs by MTT assay
Antiproliferative activity against human T47D cells after 72 hrs by MTT assay
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[PMID: 23521020] |
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.
化学情報
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CAS 番号 1429617-90-2
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性状 Solid
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分子量 546.59
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分子式 C30H29F3N6O
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Color White to light yellow
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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
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別名
DDR1-IN-2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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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Cell Death Differ
Collagen I-DDR1 signaling promotes hepatocellular carcinoma cell stemness via Hippo signaling repression. [Abstract]2023 Jul;30(7):1648-1665. PMID: 37117273 -
Cell Rep Med
Loss of p53 and SMAD4 induces adenosquamous subtype pancreatic cancer in the absence of an oncogenic KRAS mutation. [Abstract]2024 Aug 29:101711. PMID: 39232498 -
NPJ Precis Oncol
DDR1 is identified as an immunotherapy target for microsatellite stable colon cancer by CRISPR screening. [Abstract]2024 Nov 7;8(1):253. PMID: 39511298 -
J Transl Med
Inhibition of DDR1 potentiates carbon ion radiotherapy by promoting ferroptosis and immunogenic death in head and neck squamous cell carcinoma. [Abstract]2025 Sep 24;23(1):1011. PMID: 40993737 -
Oncogene
2022 Mar;41(12):1821-1834. PMID: 35140331 -
溶剤 & 溶解度
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)
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: ≥ 2.08 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.
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.
プロトコル
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (273 KB)
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SDS (393 KB)
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取扱説明書 (2659 KB)
参考文献
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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