Synonym
RU-301; RU 301; RU301
IUPAC/Chemical Name
2-(((3-Methylisoxazol-5-yl)methyl)thio)-N-(2-((3-nitro-4-(trifluoromethyl)phenyl)amino)ethyl)benzamide
InChi Key
XRFBPAPIBHOTSI-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H19F3N4O4S/c1-13-10-15(32-27-13)12-33-19-5-3-2-4-16(19)20(29)26-9-8-25-14-6-7-17(21(22,23)24)18(11-14)28(30)31/h2-7,10-11,25H,8-9,12H2,1H3,(H,26,29)
SMILES Code
O=C(NCCNC1=CC=C(C(F)(F)F)C([N+]([O-])=O)=C1)C2=CC=CC=C2SCC3=CC(C)=NO3
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
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.
In vitro activity:
RU-301 targets the extracellular domain of Axl at the interface of the Ig-1 ectodomain of Axl and the Lg-1 of Gas6. This compound effectively inhibits Gas6-inducible Axl receptor activation with low micromolar IC50s in cell-based reporter assays, curbing Gas6-induced motility in Axl-expressing cell lines.
Reference: Sci Rep. 2017 Mar 8;7:43908. https://pubmed.ncbi.nlm.nih.gov/28272423/
In vivo activity:
RU-301 suppresses H1299 lung cancer tumor growth in a mouse xenograft NOD-SCIDγ model. RU-301 exhibits potential as a pan-TAM inhibitor, as it also inhibits Gas6-inducible activation of Mertk and Tyro3. These findings emphasize RU-301's role in blocking the interface between the TAM Ig1 ectodomain and the Gas6 Lg domain, offering promising prospects for the development of small molecule Gas6-TAM interaction inhibitors as a novel class of cancer therapeutics.
Reference: Sci Rep. 2017 Mar 8;7:43908. https://pubmed.ncbi.nlm.nih.gov/28272423/
|
Solvent |
mg/mL |
mM |
comments |
| Solubility |
| DMSO |
250.0 |
520.33 |
|
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
480.46
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Sarukhanyan E, Shityakov S, Dandekar T. In Silico Designed Axl Receptor Blocking Drug Candidates Against Zika Virus Infection. ACS Omega. 2018 May 31;3(5):5281-5290. doi: 10.1021/acsomega.8b00223. Epub 2018 May 16. PMID: 30023915; PMCID: PMC6044927.
2. Kimani SG, Kumar S, Bansal N, Singh K, Kholodovych V, Comollo T, Peng Y, Kotenko SV, Sarafianos SG, Bertino JR, Welsh WJ, Birge RB. Small molecule inhibitors block Gas6-inducible TAM activation and tumorigenicity. Sci Rep. 2017 Mar 8;7:43908. doi: 10.1038/srep43908. PMID: 28272423; PMCID: PMC5341070.
In vitro protocol:
1. Sarukhanyan E, Shityakov S, Dandekar T. In Silico Designed Axl Receptor Blocking Drug Candidates Against Zika Virus Infection. ACS Omega. 2018 May 31;3(5):5281-5290. doi: 10.1021/acsomega.8b00223. Epub 2018 May 16. PMID: 30023915; PMCID: PMC6044927.
2. Kimani SG, Kumar S, Bansal N, Singh K, Kholodovych V, Comollo T, Peng Y, Kotenko SV, Sarafianos SG, Bertino JR, Welsh WJ, Birge RB. Small molecule inhibitors block Gas6-inducible TAM activation and tumorigenicity. Sci Rep. 2017 Mar 8;7:43908. doi: 10.1038/srep43908. PMID: 28272423; PMCID: PMC5341070.
In vivo protocol:
1. Kimani SG, Kumar S, Bansal N, Singh K, Kholodovych V, Comollo T, Peng Y, Kotenko SV, Sarafianos SG, Bertino JR, Welsh WJ, Birge RB. Small molecule inhibitors block Gas6-inducible TAM activation and tumorigenicity. Sci Rep. 2017 Mar 8;7:43908. doi: 10.1038/srep43908. PMID: 28272423; PMCID: PMC5341070.
1: Kimani SG, Kumar S, Bansal N, Singh K, Kholodovych V, Comollo T, Peng Y, Kotenko SV, Sarafianos SG, Bertino JR, Welsh WJ, Birge RB. Small molecule inhibitors block Gas6-inducible TAM activation and tumorigenicity. Sci Rep. 2017 Mar 8;7:43908. doi: 10.1038/srep43908. PubMed PMID: 28272423; PubMed Central PMCID: PMC5341070.
2: Sarukhanyan E, Shityakov S, Dandekar T. In Silico Designed Axl Receptor Blocking Drug Candidates Against Zika Virus Infection. ACS Omega. 2018 May 31;3(5):5281-5290. doi: 10.1021/acsomega.8b00223. Epub 2018 May 16. PubMed PMID: 30023915; PubMed Central PMCID: PMC6044927.
3: Wang, X., & Cai, B. (2020). MerTK, a risk factor for NASH fibrosis. Aging (Albany NY), 12(20), 19832.
