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Purity: ≥98%
RU-301 is a novel pan-tam inhibitor, that exerts pan-TAM inhibitory activity by binding at the interface between Gas6 and the Ig1 domain of the respective TAMs with Kd and IC50 values of 12 μM and 10 μM, respectively.
| Targets |
Axl (IC50 = 10 μM); Axl (Kd = 12 μM)
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|---|---|
| ln Vitro |
In H1299 cells, RU-301 (10 μM; 30 minutes) suppresses natural TAM activation [1]. H1299 and MDA-MB-231 cells' ability to migrate is inhibited by RU-301 (10 μM; 24 hours) [1].
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| ln Vivo |
RU-301 (intraperitoneal injection; 100–300 mg/kg; once daily for 4 days) suppresses the growth of tumors in xenograft animals [1]. In mice with NOD/SCIDγ (4-6 weeks; lung cancer xenograft model), RU-301 (300 mg/kg; i.p.; 3 times weekly) decreases liver fibrosis [1]. in ation [2].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: H1299, MDA-MB-231 cells Tested Concentrations: 10 μM (for H1299); (10 μM; 14 days) Inhibits the growth of H1299 clone-forming cells under Gas6[1]. 2.5, 5 μM (for MDA-MB-231) Incubation Duration: 30 minutes (pre-incubation) Experimental Results: Inhibition of Gas6-induced native phosphorylation of native Axl. 5 μM partially blocks Gas6-induced Akt and Erk activation in H1299 or MDA-MB-231. At 10 μM, it inhibits not only Gas6-induced native Axl phosphorylation in H1299, but also native Tyro3 and MerTK. Cell migration assay [1] Cell Types: H1299, MDA-MB-231 Cell Tested Concentrations: 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Strongly inhibited Gas6-induced motility of H1299 lung cancer cell line. Cell viability assay[1] Cell Types: H1299 Cell Tested Concentrations: 10 μM Incubation Duration: 14 days Experimental Results: Clonal growth of H1299 cells was inhibited when cultured in the presence of Gas6. |
| Animal Protocol |
Animal/Disease Models: NOD/SCIDγ mice (4-6 week; lung cancer xenograft model)[1].
Doses: 100, 300 mg/kg Route of Administration: intraperitoneal (ip) injection; single daily for 4 days Experimental Results:Dramatically diminished tumor volume while body weights were not Dramatically different. demonstrated no notable toxicity but displayed good bioavailability with a t1/2 life of ~7-8 hrs (hrs (hours)). Animal/Disease Models: WT or Mertk−/− male mice (fed NASH diet for 12 weeks) [2]. Doses: 300 mg/kg Route of Administration: intraperitoneal (ip) injection; 3 times a week for 4 weeks Experimental Results: diminished liver Sirius red staining and collagen gene expression indicated diminished liver fibrosis. |
| References |
[1]. Kimani SG, et al. Small molecule inhibitors block Gas6-inducible TAM activation and tumorigenicity. Sci Rep. 2017 Mar 8;7:43908.
[2]. Cai B, et al. Macrophage MerTK Promotes Liver Fibrosis in Nonalcoholic Steatohepatitis. Cell Metab. 2020 Feb 4;31(2):406-421.e7. |
| Molecular Formula |
C21H19F3N4O4S
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|---|---|
| Molecular Weight |
480.4622
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| Exact Mass |
480.1079
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| Elemental Analysis |
C, 52.50; H, 3.99; F, 11.86; N, 11.66; O, 13.32; S, 6.67
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| CAS # |
1110873-99-8
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| Related CAS # |
1110873-99-8
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| Appearance |
Solid powder
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| SMILES |
CC1=NOC(=C1)CSC2=CC=CC=C2C(=O)NCCNC3=C(C=C(C=C3)C(F)(F)F)[N+](=O)[O-]
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| InChi Key |
BPHPWPNHNGXNPR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H19F3N4O4S/c1-13-10-15(32-27-13)12-33-19-5-3-2-4-16(19)20(29)26-9-8-25-17-7-6-14(21(22,23)24)11-18(17)28(30)31/h2-7,10-11,25H,8-9,12H2,1H3,(H,26,29)
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| Chemical Name |
2-[(3-methyl-1,2-oxazol-5-yl)methylsulfanyl]-N-[2-[2-nitro-4-(trifluoromethyl)anilino]ethyl]benzamide
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| Synonyms |
RU-301; RU 301; RU301
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: 96~250 mg/mL (199.8~520.3 mM)
Ethanol: ~2.5 mg/mL (~5.2 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.33 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2081 mL | 1.0407 mL | 2.0813 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.
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