| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
RU-302 targets the TAM (Tyro3, Axl, Mer) receptor family, a group of receptor tyrosine kinases involved in cell survival, proliferation, and immune regulation. RU-302 binds at the interface between the TAM Ig1 ectodomain and the Gas6 ligand Lg domain, disrupting receptor dimerization and activation. By blocking Gas6-dependent TAM activation, RU-302 inhibits downstream signaling pathways including Akt and ERK activation. The compound effectively blocks Gas6-inducible Axl receptor activation with low micromolar IC50 values.
|
|---|---|
| ln Vitro |
In vitro, RU-302 effectively blocks Gas6-inducible Axl receptor activation with low micromolar IC50 values in cell assays. It potently inhibits Axl reporter cell lines and native TAM receptor cancer cell lines. The compound's ability to block TAM receptor activation has been demonstrated in various cell-based assays measuring receptor phosphorylation and downstream signaling. RU-302 is a non-selective TAM inhibitor.
|
| ln Vivo |
In vivo, RU-302 suppresses lung cancer tumor growth. The compound has been shown to effectively inhibit lung cancer tumor growth in animal models. However, specific in vivo efficacy data in animal models are not extensively detailed in the available literature. RU-302 is a research tool for studying TAM receptor signaling and its role in cancer.
|
| Enzyme Assay |
In vitro enzyme/receptor binding assays for RU-302 are not typically performed because the compound targets protein-protein interactions rather than enzyme activity. However, its binding to TAM receptors can be assessed using surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) to measure binding affinity. Competitive binding assays with labeled ligands can also be used to determine the IC50 for inhibition of Gas6 binding.
|
| Cell Assay |
In vitro cellular assays for RU-302 are performed using various cancer cell lines, including Axl reporter cell lines and native TAM receptor cancer cell lines. Cells are treated with varying concentrations of RU-302, and TAM receptor phosphorylation is assessed by Western blotting using phospho-specific antibodies. Cell viability, proliferation, and migration are assessed using standard assays. These assays confirm the compound's ability to inhibit TAM receptor activation and downstream signaling.
|
| Animal Protocol |
In vivo animal experiments for RU-302 are conducted in xenograft mouse models of lung cancer. Immunocompromised mice are implanted with human lung cancer cells and treated with RU-302 via oral or intraperitoneal administration. Tumor growth inhibition is monitored, and endpoints include tumor volume, tumor weight, and survival. Pharmacodynamic markers such as TAM phosphorylation in tumor tissues are assessed. These studies confirm the compound's anti-tumor efficacy.
|
| ADME/Pharmacokinetics |
RU-302 has a molecular weight of 475.53 and a molecular formula of C24H24F3N3O2S. The compound is a small-molecule inhibitor supplied at ≥95% purity. Detailed pharmacokinetic parameters such as half-life, Cmax, and bioavailability have not been extensively reported. As a research compound, RU-302 is primarily used in in vitro and in vivo studies to investigate TAM receptor signaling.
|
| Toxicity/Toxicokinetics |
The toxicological profile of RU-302 has not been extensively characterized. As a TAM inhibitor, RU-302 may have potential effects on immune regulation and cell survival. Standard toxicology studies would be necessary to establish its safety profile. No significant toxicity has been reported in the available research literature. The compound is a research tool and is not intended for human use.
|
| References | |
| Additional Infomation |
RU-302 is a pan-TAM receptor inhibitor that blocks the interface between the TAM Ig1 ectodomain and the Gas6 Lg domain. It effectively blocks Gas6-inducible Axl receptor activation with low micromolar IC50 values and suppresses lung cancer tumor growth. RU-302 is a non-selective TAM inhibitor and is a valuable pharmacological tool for exploring therapeutic opportunities involving TAM receptor modulation. It is a research compound and is not an approved drug.
|
| Molecular Formula |
C24H24F3N3O2S
|
|---|---|
| Molecular Weight |
475.526474952698
|
| Exact Mass |
475.154
|
| Elemental Analysis |
C, 60.62; H, 5.09; F, 11.99; N, 8.84; O, 6.73; S, 6.74
|
| CAS # |
1182129-77-6
|
| PubChem CID |
34829729
|
| Appearance |
White to off-white solid powder
|
| LogP |
5.1
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
33
|
| Complexity |
659
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC1=C(C(=NO1)C)CSC2=CC=CC=C2C(=O)N3CCN(CC3)C4=CC=CC(=C4)C(F)(F)F
|
| InChi Key |
IZHRNXCFYZERFF-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C24H24F3N3O2S/c1-16-21(17(2)32-28-16)15-33-22-9-4-3-8-20(22)23(31)30-12-10-29(11-13-30)19-7-5-6-18(14-19)24(25,26)27/h3-9,14H,10-13,15H2,1-2H3
|
| Chemical Name |
[2-[(3,5-dimethyl-1,2-oxazol-4-yl)methylsulfanyl]phenyl]-[4-[3-(trifluoromethyl)phenyl]piperazin-1-yl]methanone
|
| Synonyms |
RU302; RU 302; RU-302
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~210.29 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1029 mL | 10.5146 mL | 21.0292 mL | |
| 5 mM | 0.4206 mL | 2.1029 mL | 4.2058 mL | |
| 10 mM | 0.2103 mL | 1.0515 mL | 2.1029 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
