| 品牌 | 货号 | 产品规格 | 价格(RMB) | 库存（上海） | 北京 | 武汉 | 南京 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
| 源叶(MedMol) | S81118-2mg | 98% | ￥297.50元 | 8 | - | - | - |
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| 源叶(MedMol) | S81118-5mg | 98% | ￥501.50元 | 7 | - | - | - |
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| 源叶(MedMol) | S81118-10mg | 98% | ￥977.50元 | 7 | - | - | - |
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| 源叶(MedMol) | S81118-25mg | 98% | ￥1615.00元 | 5 | - | - | - |
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| 源叶(MedMol) | S81118-50mg | 98% | ￥2450.00元 | 预计交期：2-3天 | - | - | - |
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| 源叶(MedMol) | S81118-100mg | 98% | ￥3900.00元 | 预计交期：2-3天 | - | - | - |
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| 产品描述： Pilaralisib (XL147; SAR245408) is a potent and highly selective class I PI3Ks inhibitor with IC50s of 39 nM, 383 nM, 23 nM and 36 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ. | ||||||||||||||||||||
| 靶点： PI3Kα：39 nM (IC50)；PI3Kβ：383 nM (IC50)；PI3Kδ：36 nM (IC50)；PI3Kγ：23 nM (IC50)；Vps34：6974 nM (IC50)；DNA-PK：4750 nM (IC50);PI3K | ||||||||||||||||||||
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体内研究： The ability of Pilaralisib (XL147) to inhibit this endogenous phosphorylation of AKT, p70S6K, and S6 is examined following a single oral dose of 10, 30, 100, or 300 mg/kg. The tumors are harvested 4, 24, or 48 hours postdose and homogenized in lysis buffer. Tumor lysates from each animal (n=4) are then pooled for each group and analyzed for levels of total and phosphorylated AKT, p70S6K, and S6 by Western immunoblotting. Administration of Pilaralisib (XL147) causes a dose-dependent decrease in phosphorylation of AKT, p70S6K, and S6 in the tumors, reaching a maximum of 81% inhibition of AKT phosphorylation at 300 mg/kg at 4 hours. The dose-response relationships derived from the 4-hour time point predict 50% inhibition of AKT, p70S6K, and S6 phosphorylation at doses of approximately 100 mg/kg (pAKTT308), 54 mg/kg (pAKTS473), 71 mg/kg (p-p70S6K), and 103 mg/kg (pS6). The inhibition of AKT, p70S6K, and S6 phosphorylation in MCF7 tumors following a 100 mg/kg dose of Pilaralisib (XL147) is maximal at 4 hours, reaching 55% to 75%; however, the level of inhibition decreased to 8% to 45% by 24 hours, and only minimal or no inhibition was evident by 48 hours. Following a 300 mg/kg dose of Pilaralisib (XL147), inhibition is also maximal at 4 hours (65%-81%). However, in contrast with the 100 mg/kg dose, inhibition at 24 hours (51%-78%) is almost comparable with that seen at 4 hours, and partial inhibition (25%-51%) persisted through 48 hours |
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参考文献： 1. Foster P, et al. The Selective PI3K Inhibitor XL147 (SAR245408) Inhibits Tumor Growth and Survival and Potentiates the Activity of Chemotherapeutic Agents in Preclinical Tumor Models. Mol Cancer Ther. 2015 Apr;14(4):931-40. |
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| 溶解性： DMSO : ≥ 100 mg/mL (184.84 mM) | ||||||||||||||||||||
| 保存条件： -20℃ | ||||||||||||||||||||
配置溶液浓度参考：
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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