RU-301
Based on 1 publication(s) in Google Scholar
RU-301 is a pan TAM inhibitor that blocks Gas6-induced TAM activation and tumorigenicity. RU-301 significantly reduces nonalcoholic steatohepatitis (NASH) fibrosis, along with attenuates ERK activation and TGFβ1 expression. RU-301 can be used in studies of cancer and nonalcoholic steatohepatitis.
For research use only. We do not sell to patients.
- Purity : 99.75%
- CAS No.: 1110873-99-8
- Formula: C21H19F3N4O4S
- Molecular Weight:480.46
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) RU-301
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Biological Activity
Description
In Vitro
RU-301 (10 μM; 30 min) inhibits native TAMs activation in H1299 cells[1].
RU-301 (10 μM; 24 h) inhibits migration of H1299 and MDA-MB-231 cells[1].
RU-301 (10 μM; 14 days) inhibits growth of H1299 clonogenic cells under Gas6[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:H1299, MDA-MB-231 cells
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Concentration:10 μM (for H1299); 2.5, 5 μM (for MDA-MB-231)
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Incubation Time:30 min (pre-incubate)
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Result:Suppressed Gas6-inducible native phosphorylation of native Axl.
Partially blocked Gas6-induced activation of Akt and Erk in H1299 or MDA-MB-231 at 5 μM.
Inhibited the Gas6-induced phosphorylation of not only native Axl but also native Tyro3 and MerTK in H1299 at 10 μM.
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Cell Line:H1299, MDA-MB-231 cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Strongly suppressed Gas6-inducible motility of H1299 lung cancer cell line.
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Cell Line:H1299 cells
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Concentration:10 μM
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Incubation Time:14 days
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Result:Suppressed clonogenic growth of H1299 cells when cultured in the presence of Gas6.
In Vivo
RU-301 (300 mg/kg; i.p.; 3 times a week for 4 weeks) reduces liver fibrosis in mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCIDγ mice (4-6 week; lung cancer xenograft model)[1].
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Dosage:100, 300 mg/kg
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Administration:Intraperitoneal injection; single daily for 4 days
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Result:Significantly decreased tumor volume while body weights were not significantly different.
Showed no notable toxicity but displayed good bioavailability with a t1/2 life of ~7-8 hours.
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Animal Model:WT or Mertk−/− male mice (fed NASH diet for 12 weeks)[2].
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Dosage:300 mg/kg
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Administration:Intraperitoneal injection; 3 times a week for 4 weeks
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Result:Reduced liver fibrosis as indicated by decreases in liver picrosirius red staining and collagen gene expression.
Chemical Information
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CAS No. 1110873-99-8
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Appearance Solid
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Molecular Weight 480.46
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Formula C21H19F3N4O4S
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Color Light yellow to khaki
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SMILES
O=C(NCCNC1=CC=C(C(F)(F)F)C=C1[N+]([O-])=O)C2=CC=CC=C2SCC3=CC(C)=NO3
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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 (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (208.13 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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.33 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.
In Vivo Dissolution Calculator
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.
Protocols
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Carcinogenicity Bioassay
A carcinogenicity bioassay detects whether long-term exposure to a test substance increases benign or malignant tumor incidence, changes tumor spectrum, or shortens tumor latency in experimental animals; the classical rodent design exposes rats and/or mice to multiple dose levels for most of their lifespan, followed by complete necropsy and histopathologic diagnosis of neoplastic and non-neoplastic lesions. The readout is tumor incidence by organ, sex, species, dose group, and survival status; interpretation requires concurrent controls, dose-response assessment, survival-adjusted tumor statistics, and pathology review because mortality, spontaneous tumor background, and body-weight effects can influence apparent tumor rates.
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Fibrosis/Collagen Morphometry
Fibrosis and collagen morphometry is based on the quantitative visualization of fibrillar collagen deposition in tissue sections using histochemical stains such as Sirius Red (Picrosirius Red) or Masson's trichrome, followed by image-based or polarization-enhanced analysis to estimate collagen proportional area as a surrogate of extracellular matrix accumulation during fibrotic remodeling. Sirius Red combined with polarized light microscopy enhances detection of collagen fibers due to birefringence properties, enabling more specific visualization of collagen type I and III fibrils compared to conventional bright-field histology, while whole-section or region-restricted digital morphometry reduces field-selection bias in fibrosis assessment. Alternative quantitative approaches include second harmonic generation (SHG) and two-photon excited fluorescence microscopy, which enable label-free detection of fibrillar collagen and have been validated against histological staining and biochemica
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Collagen: Sirius Red Staining
Sirius Red or picrosirius red staining is a histochemical method for visualizing collagen-rich extracellular matrix in tissue sections, and collagen fibers are detected as red-stained structures under bright-field microscopy with enhanced birefringence under polarized light. Picrosirius red is useful for assessing total collagen organization, distribution, and fibrosis burden, but polarized color should not be interpreted as a definitive collagen type I versus type III readout because color is affected by fiber orientation, thickness, and packing.
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
Masson’s Trichrome (collagen/trichrome staining) is a histological technique that differentially stains tissue compartments using sequential acidic dyes to distinguish collagen from muscle and cytoplasmic components based on dye affinity and tissue permeability differences, enabling visualization of fibrosis and connective tissue architecture in histological sections. The classical formulation typically uses Weigert's iron hematoxylin for nuclear staining, Biebrich scarlet-acid fuchsin for cytoplasm and muscle, and aniline blue (or light green variants) for collagen, producing a characteristic blue/green collagen signal contrasted against red cytoplasm and dark nuclei. The staining principle relies on selective displacement of smaller dye molecules by larger anionic dyes in collagen-rich regions under controlled acidified conditions, which enhances collagen-specific dye retention. This property makes the method widely used for fibrosis assessment in organs such as heart, liver, lung, a
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Soft Agar Colony Formation Assay
Soft agar colony formation assay measures anchorage-independent growth, in which transformed or tumorigenic cells proliferate as colonies in a semisolid agar matrix while many non-transformed adherent cells fail to proliferate without attachment; classic studies showed that growth in semisolid medium correlates with tumorigenicity in nude mice, and later protocol papers describe the method as a stringent in vitro assay for malignant transformation. The readout is the number, size, morphology, or signal intensity of colonies formed within agar after incubation; published formats include manual colony counting after staining, 96-well or 384-well quantitative formats, DNA-binding dye detection, MTT/tetrazolium-based detection, digital image analysis, and PCR-based marker detection from soft agar cultures.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 |
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| DMSO | 1 mM | 2.0813 mL | 10.4067 mL | 20.8134 mL | 52.0335 mL |
| 5 mM | 0.4163 mL | 2.0813 mL | 4.1627 mL | 10.4067 mL | |
| 10 mM | 0.2081 mL | 1.0407 mL | 2.0813 mL | 5.2033 mL | |
| 15 mM | 0.1388 mL | 0.6938 mL | 1.3876 mL | 3.4689 mL | |
| 20 mM | 0.1041 mL | 0.5203 mL | 1.0407 mL | 2.6017 mL | |
| 25 mM | 0.0833 mL | 0.4163 mL | 0.8325 mL | 2.0813 mL | |
| 30 mM | 0.0694 mL | 0.3469 mL | 0.6938 mL | 1.7344 mL | |
| 40 mM | 0.0520 mL | 0.2602 mL | 0.5203 mL | 1.3008 mL | |
| 50 mM | 0.0416 mL | 0.2081 mL | 0.4163 mL | 1.0407 mL | |
| 60 mM | 0.0347 mL | 0.1734 mL | 0.3469 mL | 0.8672 mL | |
| 80 mM | 0.0260 mL | 0.1301 mL | 0.2602 mL | 0.6504 mL | |
| 100 mM | 0.0208 mL | 0.1041 mL | 0.2081 mL | 0.5203 mL |
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