货号	规格	价格	上海	北京	珠海	武汉
S80182-1mg	99.65%	￥110.00 S80182-1mg ￥110.00 现货	9 9	-	-	-
S80182-5mg	99.65%	￥200.00 S80182-5mg ￥200.00 现货	6 6	-	-	-
S80182-25mg	99.65%	￥650.00 S80182-25mg ￥650.00 现货	4 4	-	-	-
S80182-50mg	99.65%	￥960.00 S80182-50mg ￥960.00 现货	7 7	-	-	-
S80182-100mg	≥99%	￥1510.00 S80182-100mg ￥1510.00 2-3天	0 货期：2-3天	-	-	-

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产品描述：

Alpelisib (BYL-719) is a potent, selective, and orally active PI3Kα inhibitor. Alpelisib (BYL-719) shows efficacy in targeting PIK3CA-mutated cancer. Alpelisib (BYL-719) also inhibits p110α/p110γ/p110δ/p110β with IC50s of 5/250/290/1200 nM, respectively. Antineoplastic activity

靶点：

p110α:5 nM (IC50);p110β:1200 nM (IC50);p110δ:290 nM (IC50);p110γ:250 nM (IC50);p110α-H1047R:4 nM (IC50);p110α-E545K:4 nM (IC50);PI3K

体内研究：

Alpelisib (BYL-719) (12.5 mg/kg and 50 mg/kg for C57Bl/6J mice; 50 mg/kg for female Rj:NMRI-nude mice; oral administration; daily) significantly reduces tumor volumes and deposition of ectopic bone matrix. Alpelisib has moderate terminal elimination half-life (t1/2=2.9±0.2 h) for rat (1 mg/kg, iv)

参考文献：

1. Furet P, et al. Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3741-8. 2. Fritsch C, et al. Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials. Mol Cancer Ther. 2014 May;13(5):1117-29. 3. Gobin B, et al. BYL719, a new α-specific PI3K inhibitor: single administration and in combination with conventional chemotherapy for the treatment of osteosarcoma. Int J Cancer. 2015 Feb 15;136(4):784-96.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.265 ml	11.326 ml	22.652 ml
5 mM	0.453 ml	2.265 ml	4.53 ml
10 mM	0.227 ml	1.133 ml	2.265 ml
50 mM	0.045 ml	0.227 ml	0.453 ml

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。

参考文献

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