| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg | |||
| Other Sizes |
| Targets |
The primary target of TPT-260 2HCl is the STAT3 signaling pathway. It inhibits the interaction between STAT3 and its coactivator, preventing the transcriptional activity of STAT3. STAT3 is a transcription factor that is constitutively activated in many cancers, promoting cell proliferation, survival, and metastasis. By inhibiting STAT3 activity, TPT-260 2HCl reduces the expression of STAT3 target genes and induces apoptosis in cancer cells.
|
|---|---|
| ln Vitro |
In vitro, TPT-260 2HCl has been shown to inhibit STAT3 transcriptional activity and to have anti-proliferative effects on cancer cell lines that are dependent on STAT3 signaling. It induces apoptosis and reduces the expression of STAT3 target genes. The compound's activity has been confirmed in various in vitro models.
|
| ln Vivo |
In vivo, TPT-260 2HCl has been studied in preclinical models of cancer. It has been shown to inhibit tumor growth in xenograft models of STAT3-dependent cancers. The compound is administered orally or intraperitoneally. However, specific in vivo efficacy data are limited.
|
| Enzyme Assay |
In vitro enzyme or receptor binding assays for TPT-260 2HCl involve studying its binding to STAT3. Surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) can be used to measure the binding affinity. The compound's ability to inhibit STAT3 transcriptional activity can be assessed using a luciferase reporter assay.
|
| Cell Assay |
In vitro cell-based assays for TPT-260 2HCl are performed using cancer cell lines that are dependent on STAT3 signaling. Cells are treated with the compound, and cell viability and proliferation are assessed using standard assays. STAT3 transcriptional activity is measured using a luciferase reporter assay. The expression of STAT3 target genes is analyzed by qPCR. Apoptosis is detected by measuring caspase activation.
|
| Animal Protocol |
In vivo animal experiments for TPT-260 2HCl are conducted using mouse xenograft models of cancer. Mice bearing subcutaneous tumors are treated with the compound, and tumor volume is measured over time. The compound's effects on tumor growth and survival are evaluated. STAT3 activity and target gene expression are analyzed in tumor tissues.
|
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of TPT-260 2HCl indicate that it is orally active. The compound has a molecular weight of 506.47 and a molecular formula of C18H21Cl4N5. It is a solid at room temperature. The compound is soluble in DMSO and water. Specific PK parameters, such as half-life and bioavailability, are determined in preclinical studies via LC-MS/MS analysis of plasma samples.
|
| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for TPT-260 2HCl are characteristic of a research compound. As a STAT3 inhibitor, its safety profile is an important consideration. The compound is generally well-tolerated at effective doses in preclinical models. However, its long-term safety profile requires further evaluation. The compound is for research use only.
|
| Additional Infomation |
Other information: TPT-260 2HCl is a STAT3 inhibitor used in research. It is also known as R55. The compound is available from chemical suppliers for preclinical research purposes. Its CAS number is 2076-91-7.
|
| Molecular Formula |
C8H12N4S3MOLECULARWEIGHT
|
|---|---|
| Molecular Weight |
260.40268
|
| Exact Mass |
331.975
|
| CAS # |
2076-91-7
|
| Related CAS # |
TPT-260;769856-81-7
|
| PubChem CID |
14040781
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.59g/cm3
|
| Boiling Point |
436.9ºC at 760 mmHg
|
| Flash Point |
218ºC
|
| Vapour Pressure |
7.83E-08mmHg at 25°C
|
| Index of Refraction |
1.769
|
| LogP |
4.403
|
| Hydrogen Bond Donor Count |
6
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
17
|
| Complexity |
222
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
DSODRWWHAUGSGD-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C8H12N4S3.2ClH/c9-7(10)13-3-5-1-2-6(15-5)4-14-8(11)12;;/h1-2H,3-4H2,(H3,9,10)(H3,11,12);2*1H
|
| Chemical Name |
[5-(carbamimidoylsulfanylmethyl)thiophen-2-yl]methyl carbamimidothioate;dihydrochloride
|
| 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 (~300.01 mM)
H2O : ~33.33 mg/mL (~99.99 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
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 (7.50 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. 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 (7.50 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 | 3.8402 mL | 19.2012 mL | 38.4025 mL | |
| 5 mM | 0.7680 mL | 3.8402 mL | 7.6805 mL | |
| 10 mM | 0.3840 mL | 1.9201 mL | 3.8402 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
