TIC10 Isomer NEW
| Price | $41 | $58 | Get Latest Price |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-11 |
Product Details
| Product Name: TIC10 Isomer | CAS No.: 41276-02-2 |
| Purity: 99.25% | Supply Ability: 10g |
| Release date: 2024/11/11 |
Product Introduction
Bioactivity
| 名稱 | TIC10 Isomer |
| 描述 | TIC10 Isomer (ONC201 isomer) is an isomer of TIC10, which inactivates Akt and ERK to induce TRAIL through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Phase 1/2. |
| 體外活性 | TIC10 causes a dose-dependent increase in TRAIL mRNA and induces TRAIL protein localization on the cell surface of several cancer cell lines in a p53-independent manner. TIC10 has broad-spectrum activity against multiple malignancies in vitro and induces an increase in sub-G1 DNA content suggestive of cell death in TRAIL-sensitive HCT116 p53?/? cells, but does not alter the cell cycle profiles of normal fibroblasts at equivalent doses. TIC10 decreases the clonogenic survival of cancer cell lines and spares normal fibroblasts. TIC10 increases the percentage of sub-G1 DNA in cancer cells in a p53-independent and Bax-dependent manner, as previously reported for TRAIL-mediated apoptosis. TIC10-induced TRAIL up-regulation is Foxo3a-dependent, which also up-regulates TRAIL death receptor DR5 among other targets, potentially allowing for sensitization of some TRAIL-resistant tumor cells. TIC10 inactivates kinases Akt and extracellular signal–regulated kinase (ERK), leading to the translocation of Foxo3a into the nucleus, where it binds to the TRAIL promoter to up-regulate gene transcription. TIC10 is an efficacious antitumor therapeutic agent that acts on tumor cells and their microenvironment to enhance the concentrations of the endogenous tumor suppressor TRAIL. [1] |
| 體內(nèi)活性 | TIC10 and TRAIL treatment causes tumor regression in the HCT116 p53?/? xenograft to a comparable extent when both are administered as multiple doses. TIC10 also induces regression of MDA-MB-231 human triple-negative breast cancer xenografts, whereas TRAIL-treated tumors progressed. In DLD-1 colon cancer xenografts, TIC10 induces tumor stasis at 1 week after treatment, whereas TRAIL-treated tumors progresses after a single dose. A single dose of TIC10 also induces a sustained regression of the SW480 xenograft and is equally effective when delivered by intraperitoneal or oral route, suggesting favorable oral bioavailability for TIC10. TIC10 causes tumor-specific cell death by TRAIL-mediated direct and bystander effects. TIC10 is an effective antitumor agent against orthotopic human glioblastoma multiforme tumors. [1] |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 9 mg/mL (23.3 mM) |
| 關(guān)鍵字 | TIC-10 Isomer | Inhibitor | inhibit | TIC10 Isomer |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 抗乳腺癌化合物庫(kù) | 抗癌臨床化合物庫(kù) | 藥物功能重定位化合物庫(kù) | NO PAINS 化合物庫(kù) | 已知活性化合物庫(kù) | 抗癌化合物庫(kù) | 人代謝物化合物庫(kù) | 抗癌活性化合物庫(kù) | 抗癌藥物庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
You may like
Recommended supplier
| Product name | Price | Suppliers | Update time | |
|---|---|---|---|---|
| $496.00/1g |
VIP4Y
|
Shanghai UCHEM Inc.
|
2023-11-17 | |
| $1820.00/25mg |
VIP1Y
|
TargetMol Chemicals Inc.
|
2024-10-23 | |
| $33.00/1mg |
VIP3Y
|
TargetMol Chemicals Inc.
|
2024-11-13 |
United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
INQUIRY