TIC10 isomer (Synonyms: ONC201 isomer) |
| Catalog No.GC10350 |
TIC10 이성질체는 TIC10의 이성질체입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 41276-02-2
Sample solution is provided at 25 µL, 10mM.
TIC10 (TRAIL-inducing compound 10) is a potent and stable small molecule that is orally active. It induces TRAIL transcriptionally independent of p53 and crosses the blood-brain barrier. [1]
Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) is an apoptosis inducer in a variety of human cancer cell lines. It also acts as a tumor suppressor during immune surveillance but the function is lost in cancer progression. [1]
TIC10 caused a prominent and long-lasting production of TRAIL on cell surface of tumor cell.
TIC10 also led to TRAIL-mediated apoptosis in HCT116 p53-/- cells. In addition, TIC10 inactivated Akt and ERK cooperatively lead to the nuclear translocation of Foxo3a and ensuing TRAIL up-regulation. [1]
In mouse caner xenograft, TIC10 showed TRAIL-dependent antitumor effect. It caused tumor-specific cell death by RAIL-mediated direct and bystander effects. TIC10 is also an effective antitumor agent for orthotopic human glioblastoma multiforme tumors. [1]
Reference:
1. Allen JE, Krigsfeld G, Mayes PA et al. Dual inactivation of Akt and ERK by TIC10 signals Foxo3a nuclear translocation, TRAIL gene induction, and potent antitumor effects. Sci Transl Med. 2013 Feb 6;5(171):171ra17.
| Cell experiment [1]: | |
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Cell lines |
HCT116 Bax-/- and HCT116 p53-/- cells |
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Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
1.25, 2.5, 5 and 10 μM; 24, 48 or 72 hours |
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Applications |
In TRAIL-sensitive HCT116 p53-/- cells, TIC10 induced an increase in sub-G1 DNA content suggestive of cell death in a p53-independent and Bax-dependent manner. In TRAIL-resistant Bax-null HCT116 human colon cancer cells, TIC10 (10 μM, 72 h) dose-dependently increased TRAIL mRNA and induced TRAIL protein localization on the cell surface in a p53-independent manner. |
| Animal experiment [2]: | |
|
Animal models |
Female athymic nu/nu mice subcutaneous xenografted with HCT116 p53-/- tumor and MDA-MB-231 human triple-negative breast cancer. |
|
Dosage form |
50, 80 or 100 mg/kg; intraperitoneal injection; administered on days 0, 3, and 6 |
|
Application |
In mice bearing the HCT116 p53-/- xenograft, TIC10 caused tumor regression. TIC10 also induced regression of MDA-MB-231 human triple-negative breast cancer xenografts. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Allen JE, Krigsfeld G, Mayes PA et al. Dual inactivation of Akt and ERK by TIC10 signals Foxo3a nuclear translocation, TRAIL gene induction, and potent antitumor effects. Sci Transl Med. 2013 Feb 6;5(171):171ra17. |
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| Cas No. | 41276-02-2 | SDF | |
| Synonyms | ONC201 isomer | ||
| Chemical Name | 7-benzyl-10-(2-methylbenzyl)-2,3,6,7,8,9-hexahydroimidazo[1,2-a]pyrido[4,3-d]pyrimidin-5(10H)-one | ||
| Canonical SMILES | O=C1C(CN(CC2=CC=CC=C2)CC3)=C3N(CC4=CC=CC=C4C)C5=NCCN15 | ||
| Formula | C24H26N4O | M.Wt | 386.49 |
| Solubility | ≥ 6.43mg/mL in DMSO with gentle warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5874 mL | 12.9369 mL | 25.8739 mL |
| 5 mM | 0.5175 mL | 2.5874 mL | 5.1748 mL |
| 10 mM | 0.2587 mL | 1.2937 mL | 2.5874 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)
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