1. Protein Tyrosine Kinase/RTK
  2. TAM Receptor
  3. RU-301

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.

RU-301 Chemical Structure

RU-301 Chemical Structure

CAS No. : 1110873-99-8

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 328 In-stock
Solution
10 mM * 1 mL in DMSO USD 328 In-stock
Solid
1 mg USD 147 In-stock
5 mg USD 310 In-stock
10 mg USD 490 In-stock
25 mg USD 890 In-stock
50 mg USD 1400 In-stock
100 mg USD 2000 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

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 t1/2 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.
Molecular Weight

480.46

Formula

C21H19F3N4O4S

CAS No.
Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0813 mL 10.4067 mL 20.8134 mL
5 mM 0.4163 mL 2.0813 mL 4.1627 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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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.

  • 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.

    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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(per animal)

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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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+
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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 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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RU-301 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
RU-301
Cat. No.:
HY-119039
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