2. PROTAC Protein Tyrosine Kinase/RTK
  3. Molecular Glues Anaplastic lymphoma kinase (ALK)
  4. TRI-611

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.

For research use only. We do not sell to patients.

TRI-611

TRI-611 Chemical Structure

CAS No. : 3117940-39-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
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10 mg In-stock
25 mg In-stock
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100 mg In-stock
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Based on 1 publication(s) in Google Scholar

TRI-611 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3].

In Vitro

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 Related Antibodies
In Vivo

In mouse efficacy studies, TRI-611 leads to the regression of subcutaneous xenografts of CRISPR engineered EML4-ALK-mutant NCI-H3122 cells that do not respond to ALK TKIs[1].
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.
Molecular Weight

404.38

Formula

C21H16N4O5
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4729 mL 12.3646 mL 24.7292 mL
5 mM 0.4946 mL 2.4729 mL 4.9458 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
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TRI-611 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TRI-6113117940-39-0TRI611TRI 611Molecular GluesAnaplastic lymphoma kinase (ALK)Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246ALK-positive cancer cellsEML4-ALK mutant proteinsanaplastic lymphoma kinase (ALK)non-small cell lung cancerNTRK family kinasesALK L1196M/G1202R compound mutant proteinsCRL4CRBN E3 ligasecentral nervous system metastasesBa/F3 cellsCRBNInhibitorinhibitorinhibit

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