Art. -Nr.: HY-119039

RU-301

1 Cited Publications

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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.

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Reinheit: 99.75%
CAS. Nr.: 1110873-99-8
Formel: C₂₁H₁₉F₃N₄O₄S
Molecular Weight:480.46

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

RU-301 Chemical Structure

CAS. Nr.: 1110873-99-8

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle TAM Receptor Isoform-spezifische Produkte anzeigen :

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.

Cell Viability Assay^[1]

Cell Line:

H1299, MDA-MB-231 cells
Concentration:

10 μM (for H1299); 2.5, 5 μM (for MDA-MB-231)
Incubation Time:

30 min (pre-incubate)
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.

Cell Migration Assay ^[1]

Cell Line:

H1299, MDA-MB-231 cells
Concentration:

10 μM
Incubation Time:

24 h
Result:

Strongly suppressed Gas6-inducible motility of H1299 lung cancer cell line.

Cell Viability Assay ^[1]

Cell Line:

H1299 cells
Concentration:

10 μM
Incubation Time:

14 days
Result:

Suppressed clonogenic growth of H1299 cells when cultured in the presence of Gas6.

In Vivo

RU-301 (100, 300 mg/kg; i.p.; single daily for 4 days) inhibits tumor growth in lung cancer xenograft model^[1].
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.

Animal Model:

NOD/SCIDγ mice (4-6 week; lung cancer xenograft model)^[1].
Dosage:

100, 300 mg/kg
Administration:

Intraperitoneal injection; single daily for 4 days
Result:

Significantly decreased tumor volume while body weights were not significantly different.
Showed no notable toxicity but displayed good bioavailability with a t_1/2 life of ~7-8 hours.

Animal Model:

WT or Mertk^−/− male mice (fed NASH diet for 12 weeks)^[2].
Dosage:

300 mg/kg
Administration:

Intraperitoneal injection; 3 times a week for 4 weeks
Result:

Reduced liver fibrosis as indicated by decreases in liver picrosirius red staining and collagen gene expression.

Chemical Information

CAS. Nr. 1110873-99-8
Appearance Solid
Molecular Weight 480.46
Formel C₂₁H₁₉F₃N₄O₄S
Color Light yellow to khaki
SMILES

O=C(NCCNC1=CC=C(C(F)(F)F)C=C1[N+]([O-])=O)C2=CC=CC=C2SCC3=CC(C)=NO3
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

bioRxiv

2024 August 06.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0813 mL

10.4067 mL

20.8134 mL

5 mM

0.4163 mL

2.0813 mL

4.1627 mL

10 mM

0.2081 mL

1.0407 mL

2.0813 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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: ≥ 2.08 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Kimani SG, et al. Small molecule inhibitors block Gas6-inducible TAM activation and tumorigenicity. Sci Rep. 2017 Mar 8;7:43908. [Content Brief]

[2]. Cai B, et al. Macrophage MerTK Promotes Liver Fibrosis in Nonalcoholic Steatohepatitis. Cell Metab. 2020 Feb 4;31(2):406-421.e7. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	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

Keywords

RU-301

1 Cited Publications

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RU-301

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Anti-Lung Cancer Compound Library

Targeted Diversity Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) RU-301

Alle TAM Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

RU-301

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Anti-Lung Cancer Compound Library

Targeted Diversity Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) RU-301

Alle TAM Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

RU-301 Related Classifications

HY-119039 Related Classifications