Sapanisertib NEW
| Price | $34 | $47 | $77 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-16 |
Product Details
| Product Name: Sapanisertib | CAS No.: 1224844-38-5 |
| Purity: 99.34% | Supply Ability: 10g |
| Release date: 2024/11/16 |
Product Introduction
Bioactivity
| 名稱 | Sapanisertib |
| 描述 | Sapanisertib (INK 128) is an orally bioavailable inhibitor of raptor-mTOR (TOR complex 1 or TORC1) and rictor-mTOR (TOR complex 2 or TORC2) with potential antineoplastic activity. |
| 細(xì)胞實(shí)驗(yàn) | PC3 cells are treated with the appropriate drug for 48 h, and proliferation is measured using CellTiter-Glo Luminescent reagent. The concentration of INK128 necessary to achieve inhibition of cell growth by 50% (IC50) is calculated using concentrations ranging from 20.0 μM to 0.1 nM (12-point curve). |
| 激酶實(shí)驗(yàn) | mTOR activity is assayed using LanthaScreen Kinase kit reagents. PI(3)K α, β, γ and δ activity are assayed using the PI(3)K HTRF assay kit. The concentration of INK128 necessary to achieve inhibition of enzyme activity by 50% (IC50) is calculated using concentrations ranging from 20 μM to 0.1 nM (12-point curve). IC50?values are determined using a nonlinear regression model. |
| 體外活性 | Administering INK 128 orally on a daily basis to various transplant model systems inhibits angiogenesis and tumor growth. Daily treatment of the ZR-75-1 breast cancer xenograft model with 0.3 mg/kg of INK 128 demonstrated a suppressive effect on tumor growth. |
| 體內(nèi)活性 | INK 128 functions as a dual inhibitor of TORC1/2, suppressing the phosphorylation of TORC1's downstream substrates S6 and 4EBP1, while selectively inhibiting the phosphorylation of AKT on Ser473, a downstream substrate of TORC2. It exhibits enzymatic inhibitory activity against mTOR, presenting over 100-fold selectivity towards PI3K kinases. Moreover, INK 128 effectively inhibits cell lines resistant to rapamycin and pan-PI3K inhibitors. |
| 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 | Ethanol : 2 mg/mL (6.46 mM) DMSO : 18.33 mg/mL (59.27 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) |
| 關(guān)鍵字 | MLN 0128 | INK128 | inhibit | TAK 228 | INK-128 | Sapanisertib | TAK228 | Autophagy | Mammalian target of Rapamycin | MLN-0128 | mTOR | Inhibitor |
| 相關(guān)產(chǎn)品 | Stavudine | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Curcumin | Oxyresveratrol | Paeonol | Naringin | Gefitinib |
| 相關(guān)庫(kù) | 高選擇性抑制劑庫(kù) | 經(jīng)典已知活性庫(kù) | 激酶抑制劑庫(kù) | 抗癌臨床化合物庫(kù) | 藥物功能重定位化合物庫(kù) | 抑制劑庫(kù) | 抗衰老化合物庫(kù) | 已知活性化合物庫(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.
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