| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| Other Sizes |
| Targets |
Thyroid hormone receptor interacting protein 13 (Trip13)[1]
TI17 specifically targets Trip13 (Thyroid hormone Receptor-Interacting Protein 13), an AAA-ATPase that plays a critical role in DNA double-strand break (DSB) repair and maintenance of genomic stability. By inhibiting Trip13, TI17 impairs the cell‘s ability to repair DNA damage, leading to cell death. |
|---|---|
| ln Vitro |
TI17 effectively inhibits the proliferation of multiple myeloma (MM) cell lines in vitro. Treatment with TI17 induces cell cycle arrest and apoptosis in MM cells. It increases DNA damage by impairing Trip13-mediated DSB repair, which leads to the accumulation of DNA damage and subsequently triggers programmed cell death.
|
| ln Vivo |
In vivo data for this compound is currently not available for public reference. As an inhibitor of a DNA repair protein, TI17 is being investigated for its potential to enhance the efficacy of DNA-damaging chemotherapies and to treat cancers that are reliant on Trip13 function.
|
| Enzyme Assay |
Cell-free assays for Trip13 inhibition measure ATPase activity. Recombinant Trip13 protein is incubated with ATP and varying concentrations of TI17. The amount of inorganic phosphate released from ATP hydrolysis is measured using a colorimetric assay (e.g., malachite green), and the half-maximal inhibitory concentration (IC50) for the inhibition of ATPase activity is calculated.
|
| Cell Assay |
Cellular assays are conducted in multiple myeloma (MM) cell lines. Cells are treated with TI17 for 24-72 hours. Cell proliferation is measured using a CCK-8 or MTT assay. Cell cycle distribution is analyzed by flow cytometry with propidium iodide (PI) staining, and apoptosis is quantified using Annexin V/PI double staining. DNA damage is assessed by immunoblotting for gamma-H2AX, a marker of DSBs.
|
| Animal Protocol |
In vivo data is not available for this research compound. As a laboratory chemical for cell-based and in vitro studies, it is not typically formulated for animal pharmacokinetic or efficacy studies in a standard research setting.
|
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties are not documented. As a laboratory chemical primarily for in vitro use, ADME (Absorption, Distribution, Metabolism, Excretion) data are not typically required or reported.
|
| Toxicity/Toxicokinetics |
Toxicological and safety profiles have not been formally established. This compound is intended for research use only and is not for human consumption. Standard safety precautions for handling bioactive small molecules and fine chemicals should be followed.
|
| References | |
| Additional Infomation |
TI17 is a potent inhibitor of TRIP13, a protein often overexpressed in various cancers to help them resist chemotherapy. As a new class of anti-cancer agent, TI17 is a valuable chemical probe to study the role of TRIP13 in DNA repair and to evaluate its potential as a therapeutic target for combination therapy in multiple myeloma and other solid tumors.
|
| CAS # |
1005178-02-8
|
|---|---|
| Appearance |
White to off-white solid powder
|
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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.