TRI-611
Based on 1 Customer Validation
TRI-611 is a brain-penetrant, orally active molecular glue degrader targeting ALK. TRI-611 engages ALK via a distal degron, forms a ternary complex with CRBN, triggers ALK polyubiquitination and degradation, including TKI-resistant ALK fusion proteins. TRI-611 inhibits ALK downstream signaling pathways, induces anti-proliferative effects in ALK-positive cancer cells. TRI-611 induces regression of ALK-positive non-small cell lung cancer tumors in preclinical xenograft models. TRI-611 can be used for the research of ALK-positive non-small cell lung cancer, including TKI-refractory tumors and central nervous system metastases.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.07%
- No. CAS: 3117940-39-0
- Fòrmula: C21H16N4O5
- Peso molecular:404.38
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
TRI-611 equally effectively promotes CRBN interaction and subsequent poly-ubiquitination of both wild-type ALK and ALKL1196M/G1202R compound mutant proteins in cell-free biochemical/biophysical assays[1].
TRI-611 effectively targets all 30 tested EML4-ALK mutant proteins, including TKI-refractory variants, in engineered Ba/F3 cells[1].
TRI-611 potently inhibits the proliferation of ALK-positive NSCLC cell line carrying multiple ALK TKI resistance alleles[1].
TRI-611 induces rapid, robust, and durable CRBN-dependent degradation of EML4-ALK fusion protein and oncogenic transmembrane ALK in ALK-positive cells, with >90% maximum degradation achieved within 1-2 hours and a recovery half-life of more than 15 hours after compound withdrawal[2].
TRI-611 promotes ubiquitination and degradation of ALK fusion alleles (including TKI-resistant variants) and exerts a broader phenotypic impact on ALK fusion-driven NSCLC cell lines than ALK TKIs[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
TRI-611 is orally bioavailable and brain penetrant, with daily oral dosing leading to deep and durable degradation of endogenous EML4-ALK and tumor regression in both subcutaneous and intracranial xenograft models of ALK-positive NSCLC[2][3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
No. CAS 3117940-39-0
-
Appearance Solid
-
Peso molecular 404.38
-
Fòrmula C21H16N4O5
-
Color White to off-white
-
SMILES
O=C(O1)N(C2CCC(NC2=O)=O)C3=C1C=CC(CC4=NC(C5=CC=CC=C5)=NO4)=C3
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (247.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.18 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.18 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
-
Ficha de datos (277 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4729 mL | 12.3646 mL | 24.7292 mL | 61.8230 mL |
| 5 mM | 0.4946 mL | 2.4729 mL | 4.9458 mL | 12.3646 mL | |
| 10 mM | 0.2473 mL | 1.2365 mL | 2.4729 mL | 6.1823 mL | |
| 15 mM | 0.1649 mL | 0.8243 mL | 1.6486 mL | 4.1215 mL | |
| 20 mM | 0.1236 mL | 0.6182 mL | 1.2365 mL | 3.0912 mL | |
| 25 mM | 0.0989 mL | 0.4946 mL | 0.9892 mL | 2.4729 mL | |
| 30 mM | 0.0824 mL | 0.4122 mL | 0.8243 mL | 2.0608 mL | |
| 40 mM | 0.0618 mL | 0.3091 mL | 0.6182 mL | 1.5456 mL | |
| 50 mM | 0.0495 mL | 0.2473 mL | 0.4946 mL | 1.2365 mL | |
| 60 mM | 0.0412 mL | 0.2061 mL | 0.4122 mL | 1.0304 mL | |
| 80 mM | 0.0309 mL | 0.1546 mL | 0.3091 mL | 0.7728 mL | |
| 100 mM | 0.0247 mL | 0.1236 mL | 0.2473 mL | 0.6182 mL |
TRI-611 Related Classifications
HY-183116 Related Classifications
Powered by Bioz
- TRI-611
- 3117940-39-0
- TRI611
- TRI 611
- Molecular Glues
- Anaplastic lymphoma kinase (ALK)
- ALK-positive cancer cells
- EML4-ALK mutant proteins
- anaplastic lymphoma kinase (ALK)
- non-small cell lung cancer
- NTRK family kinases
- ALK L1196M/G1202R compound mutant proteins
- CRL4CRBN E3 ligase
- central nervous system metastases
- Ba/F3 cells
- CRBN
- Inhibitor
- inhibitor
- inhibit