| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg | |||
| Other Sizes |
| Targets |
(R)-UT-155 targets the androgen receptor (AR), a nuclear receptor that plays a critical role in prostate cancer progression. As a selective androgen receptor degrader (SARD), (R)-UT-155 binds to the amino-terminal transcriptional activation domain AF-1 of the AR. The compound markedly reduces the activity of both wild-type and splice variant isoforms of AR. By binding to AR and promoting its degradation, (R)-UT-155 blocks androgen receptor signaling, which is a key driver of prostate cancer growth.
|
|---|---|
| ln Vitro |
In vitro, (R)-UT-155 functions as a selective androgen receptor degrader (SARD) ligand. The compound binds to the amino-terminal transcriptional activation domain AF-1 of the androgen receptor and markedly reduces the activity of wild-type and splice variant isoforms of AR. The R-isomer is reported to be less active than the S-isomer. These in vitro properties establish (R)-UT-155 as a valuable research tool for studying AR biology and degradation mechanisms.
|
| ln Vivo |
Detailed in vivo activity data for (R)-UT-155 are limited in publicly available literature. As a selective androgen receptor degrader, the compound is being investigated for its potential in prostate cancer research. Its ability to reduce the activity of both wild-type and splice variant AR isoforms suggests potential for overcoming resistance to standard androgen deprivation therapies. Further in vivo studies are needed to fully characterize its therapeutic potential.
|
| Enzyme Assay |
(R)-UT-155 is not typically used in standard receptor binding assays. Its activity is assessed through cell-based assays measuring androgen receptor degradation and signaling. In these assays, cells expressing wild-type or mutant AR are treated with (R)-UT-155 at varying concentrations. AR protein levels are assessed by Western blot. AR transcriptional activity is assessed using reporter gene assays measuring AR-dependent transcription. Cell viability and proliferation are assessed using standard assays such as MTT or CellTiter-Glo.
|
| Cell Assay |
Cellular assays for (R)-UT-155 are performed using prostate cancer cell lines that express androgen receptor, such as LNCaP or VCaP cells. Cells are cultured in appropriate media and treated with (R)-UT-155 at varying concentrations for defined time periods. AR protein levels are assessed by Western blot to determine the extent of AR degradation. AR transcriptional activity is assessed by measuring the expression of AR target genes by qRT-PCR or by using AR-dependent reporter gene assays. Cell viability and proliferation are assessed using standard assays such as MTT or CellTiter-Glo.
|
| Animal Protocol |
In vivo studies with (R)-UT-155 are conducted in mouse xenograft models using prostate cancer cell lines. (R)-UT-155 is administered via appropriate routes (e.g., intraperitoneal or oral) at defined doses and schedules. Tumor growth is monitored by caliper measurements, and tumor volumes are calculated. Tumor tissues are collected for assessment of AR protein levels and signaling pathway modulation by Western blot or immunohistochemistry. Pharmacokinetic parameters are determined from plasma samples collected at various time points.
|
| ADME/Pharmacokinetics |
(R)-UT-155 has a molecular weight of 405.35 and a molecular formula of C20H15F4N3O2. The compound is a selective androgen receptor degrader (SARD) ligand. Detailed pharmacokinetic data for (R)-UT-155 are not extensively documented in publicly available literature. The compound is soluble in DMSO. It should be stored at -20degC. The R-isomer is reported to be less active than the S-isomer.
|
| Toxicity/Toxicokinetics |
Comprehensive toxicology data for (R)-UT-155 are not extensively documented in publicly available sources. The compound is intended for research use only and is not approved for human therapeutic applications. Standard laboratory safety practices should be followed when handling this compound, including the use of appropriate personal protective equipment and adherence to institutional biosafety and chemical hygiene guidelines. The compound has a purity of ≥98%.
|
| References | |
| Additional Infomation |
(R)-UT-155 is a selective androgen receptor degrader (SARD) ligand that markedly reduces the activity of wild-type and splice variant isoforms of the androgen receptor by binding to the amino-terminal transcriptional activation domain AF-1. The compound has a molecular weight of 405.35 and a molecular formula of C20H15F4N3O2. The R-isomer is less active than the S-isomer. (R)-UT-155 is for research purposes only.
|
| Molecular Formula |
C20H15F4N3O2
|
|---|---|
| Molecular Weight |
405.345618486404
|
| Exact Mass |
405.11
|
| CAS # |
2031161-54-1
|
| Related CAS # |
UT-155;2031161-35-8
|
| PubChem CID |
122640149
|
| Appearance |
White to off-white solid powder
|
| LogP |
3.1
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
29
|
| Complexity |
664
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
FC1C=CC2=C(C=1)C=CN2C[C@@](C(NC1C=CC(C#N)=C(C(F)(F)F)C=1)=O)(C)O
|
| InChi Key |
CFSAYQVTXBMPRF-LJQANCHMSA-N
|
| InChi Code |
InChI=1S/C20H15F4N3O2/c1-19(29,11-27-7-6-12-8-14(21)3-5-17(12)27)18(28)26-15-4-2-13(10-25)16(9-15)20(22,23)24/h2-9,29H,11H2,1H3,(H,26,28)/t19-/m1/s1
|
| Chemical Name |
(2R)-N-[4-cyano-3-(trifluoromethyl)phenyl]-3-(5-fluoroindol-1-yl)-2-hydroxy-2-methylpropanamide
|
| 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 (~246.70 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.17 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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. Solubility in Formulation 2: 2.5 mg/mL (6.17 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4670 mL | 12.3350 mL | 24.6700 mL | |
| 5 mM | 0.4934 mL | 2.4670 mL | 4.9340 mL | |
| 10 mM | 0.2467 mL | 1.2335 mL | 2.4670 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
