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- CAS号：
1217486-61-7
- 规格：
1mg/1mLx10mM(inDMSO)/2mg/5mg/10mg/25mg/50mg/100mg/200mg
| 规格： | 1mg | 产品价格： | ￥223.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥553.0 |
| 规格： | 2mg | 产品价格： | ￥308.0 |
| 规格： | 5mg | 产品价格： | ￥472.0 |
| 规格： | 10mg | 产品价格： | ￥784.0 |
| 规格： | 25mg | 产品价格： | ￥1400.0 |
| 规格： | 50mg | 产品价格： | ￥2224.0 |
| 规格： | 100mg | 产品价格： | ￥3104.0 |
| 规格： | 200mg | 产品价格： | ￥4440.0 |
Product Introduction
Bioactivity
| 名称 | Alpelisib |
| 描述 | Alpelisib (BYL-719) is a PI3Kα inhibitor (IC50=5 nM) with selective, potent, and oral activity. Alpelisib inhibits PI3Kβ/γ/δ with low activity (IC50=250/290/1200 nM). Alpelisib has antitumor activity and is targeted to PIK3CA mutant tumors. |
| 细胞实验 | To evaluate the isoform-specific potency of NVP-BYL719 in a cell-based system, an N-terminally myristoylated form of each PI3K class IA isoform was expressed in Rat1 fibroblasts. The retroviral expression plasmid pBabePuro containing human p110α, p110β, and p110δ with an N-terminal myristoylation (myr) signal followed by an HA-tag were generated. Successfully infected Rat1 cells were selected in medium containing 4 μg/mL of puromycin, expanded and characterized for expression of the p110 isoforms. Transgenic expression of the myristoylated protein was confirmed by increased levels of phosphorylated Akt [1]. |
| 动物实验 | All in life experimentation and efficacy studies were conducted as described previously. Tumor xenografts were grown subcutaneously or orthotopically in nude mice or nude Rowett rats (Hsd: RH-Fox1rnu) by injection of 3 × 10^6 to 1 × 10^7 cells or implantation of tumor fragments of approximately 50 mg. Tumor-bearing animals mice were treated with either vehicle control, NVP-BYL719, or NVP-BKM120 (p.o., every day) at the doses indicated [1]. |
| 体外活性 | 方法：骨肉瘤细胞系 MG-63、HOS、MOS-J 和 POS-1 用 Alpelisib (0-50 µM) 处理 72 h，使用 XTT assay 检测细胞活力。 结果：Alpelisib 以剂量依赖性方式显著抑制所有骨肉瘤细胞系的细胞生长，IC50 范围为 6-15 µM，IC90 范围为 24-42 µM。[1] 方法：PIK3CA 野生型细胞 (SNU638 和 SNU668) 和三个 PIK3CA 突变体细胞 (SNU601、AGS 和 MKN1) 用 Alpelisib (5 µM) 处理 24 h，使用 Flow cytometry 检测细胞周期情况。 结果：无论 PIK3CA 突变状态如何，Alpelisib 处理都诱导 G0/G1 细胞周期停滞。在 PIK3CA 突变细胞 (AGS 和 MKN1) 中，亚 G1 组分显著增加，表明 Alpelisib 在这些细胞系中增加了细胞凋亡。[2] |
| 体内活性 | 方法：为检测体内抗肿瘤活性，将 Alpelisib (12.5-50 mg/kg，methylcellulose 0.5%) 口服给药给携带人骨肉瘤 HOS-MNNG 的 Rj:NMRI-nude 小鼠，每天一次，持续二十二天。 结果：Alpelisib 以剂量依赖性方式显著减少肿瘤体积。[1] 方法：为研究对胶原蛋白的调节作用，将 Alpelisib (12.5-50 mg/kg) 口服给药给携带 Rat1-myr-p110α 肿瘤皮下异种移植的 nude 小鼠，每天一次，持续八天。 结果：12.5、25、50 mg/kg 的 Alpelisib 治疗具有良好的耐受性，并产生了剂量依赖性和统计学上显著的抗肿瘤效果，T/C 为 14.1%，消退为 9.6% 和 65.2%。[3] |
| 存储条件 | Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 240 mg/mL (543.64 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 8.2 mg/mL (18.57 mM), Suspension. Ethanol : 2 mg/mL (4.53 mM), Sonication is recommended. |
| 关键字 | PIK3CA | PI3Kα | PI3K | phosphorylation | Phosphoinositide 3-kinase | p110α | mutant | metastasis | Inhibitor | inhibit | cancer | BYL719 | BYL 719 | breast | antineoplastic | Alpelisib | AKT |
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| 相关库 | Anti-Cancer Approved Drug Library | Bioactive Compound Library | Bioactive Compounds Library Max | EMA Approved Drug Library | Kinase Inhibitor Library | Anti-Aging Compound Library | FDA-Approved Drug Library | Immunology/Inflammation Compound Library | FDA-Approved Kinase Inhibitor Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |
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￥223 - 4440
