| 名稱 | Pilaralisib |
| 描述 | Pilaralisib (XL-147) is an orally available small molecule that selectively inhibits the activity of phosphoinositide-3 kinase (PI3K). Pilaralisib has been used in trials studying the treatment of Cancer, Lymphoma, Solid Tumors, Glioblastoma, and Breast Cancer, among others. |
| 細(xì)胞實(shí)驗(yàn) | Cell proliferation is measured by using MTT or pre-mixed WST-1 reagent. For MTT/WST-1 assays, 10,000 cells/well are seeded in 96-well plates. 24 h after plating, cells are treated with DMSO or pilaralisib. After 5 days of treatment, MTT/WST-1 assays are performed.(Only for Reference) |
| 激酶實(shí)驗(yàn) | In vitro kinase inhibition assays: Kinase activity for PI3K isoforms is measured as the percentage of ATP consumed following the kinase reaction using luciferase–luciferin-coupled chemiluminescence, with ATP concentrations approximately equal to the Km for each respective kinase. Kinase reactions are initiated by combining test compounds, ATP and kinase in a 20 μL volume. PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ final enzyme concentrations are 0.5, 8, 20, and 2 nM, respectively. Of note, 0.5 μL dimethyl sulfoxide (DMSO) containing varying concentrations of the test compound is mixed with 10 μL enzyme solution (2×concentration). Kinase reactions are initiated by the addition of 10 μL of liver phosphatidylinositol and ATP solution (2×concentration). Assay concentrations for VPS34, ATP, and phosphatidylinositol are 40 nM, 1 μM, and 5 μM, respectively |
| 體外活性 | Pilaralisib 在小兒臨床前測(cè)試計(jì)劃 (PPTP) 細(xì)胞系展示出細(xì)胞毒活性，中位相對(duì)IC50值為10.9 mM（范圍從2.7 mM到24.5 mM）。[2] |
| 體內(nèi)活性 | 在 BALB/c nu/nu 小鼠中，Pilaralisib（100 mg/kg，p.o.）能有效抑制實(shí)體膠質(zhì)瘤異種移植物的生長(zhǎng)。Pilaralisib 的耐受性良好，治療組的毒性率僅為0.7%。[2] 在無(wú)胸腺雌性小鼠中，Pilaralisib（100 mg/kg，p.o.）顯著延緩腫瘤生長(zhǎng)，且未觀察到顯著的藥物相關(guān)毒性。[3] |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | Ethanol : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 6.25 mg/mL (11.55 mM), Solution.
10% DMSO+90% Saline : < 6.25 mg/mL (11.55 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.
DMSO : 62.5 mg/mL (115.52 mM), Sonication is recommended.
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| 關(guān)鍵字 | XL147 | XL 147 | SAR-245408 | SAR 245408 | Pilaralisib | PI3Kδ | PI3Kγ | PI3Kβ | PI3Kα | PI3K | Phosphoinositide 3-kinase | Inhibitor | inhibit |
| 相關(guān)產(chǎn)品 | 4-Methylbenzylidene camphor | Berberine hydrogen sulphate | Creatine monohydrate | Musk ketone | Quercetin | Hyaluronic acid | Berberine sulfate | Methyl eugenol | Myricetin | Quercitrin hydrate | Isoprenaline hydrochloride | 4-Vinylcyclohexene Dioxide |
| 相關(guān)庫(kù) | 抑制劑庫(kù) | 抗癌活性化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 已知活性化合物庫(kù) | ReFRAME 相關(guān)化合物庫(kù) | 激酶抑制劑庫(kù) | 抗衰老化合物庫(kù) | 免疫/炎癥分子化合物庫(kù) | 藥物功能重定位化合物庫(kù) | 抗癌臨床化合物庫(kù) | PI3K/Akt/mTOR 化合物庫(kù) | 抗癌藥物庫(kù) |