Alpelisib (BYL719)

製品コードS2814 バッチS281404

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₉H₂₂F₃N₅O₂S

分子量

441.47

CAS No.

1217486-61-7

Solubility (25°C)*

体外

DMSO

88 mg/mL (199.33 mM)

Ethanol (warmed with 50ºC water bath)

2 mg/mL (4.53 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	アルペリシブ (Alpelisib (BYL719)) はPI3Kβ/γ/δ に対する影響が最小限の、強力かつ選択的な PI3Kα 阻害剤(無細胞アッセイで IC50 = 5 nM) です。臨床フェーズ2。
in vitro	Alpelisib (BYL719) inhibits the proliferation of breast cancer cell lines harboring PIK3CA mutations, correlating with inhibition of various downstream signaling components of the PI3K/Akt pathway. ^[1]
in vivo	Alpelisib (BYL719) shows statistically significant dose-dependent anti-tumor efficacy in PIK3CA mutant xenograft models in rodents at doses exceeding 270 mg/d. It has a low clearance, a half-life of 8.5 h and its exposure increases dose proportionally between 30mg/d and 450mg/d, displaying a low inter-individual variability in Cmax and AUC in human. At 270mg/d, this compound shows first signs of clinical efficacy include 1 confirmed partial response in a patient with ER+ breast cancer, and significant PET responses (PMR) and/or tumor shrinkage are achieved in 8 out of 17 evaluated patients. ^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	CW2 cells
	濃度	500 nM
	反応時間	72 h
	実験の流れ	Cells were treated with increasing concentrations of alpelisib (BYL719) (0–1000 nM) for 72 h, and cell viability was quantified using the CyQuant assay.
動物実験	動物モデル	Female athymic nu/nu mice
	投薬量	40 mg/kg
	投与方法	o.g.

参考

http://cancerres.aacrjournals.org/cgi/content/short/72/8_MeetingAbstracts/CT-01?rss=1
https://pubmed.ncbi.nlm.nih.gov/34171264/

カスタマーフィードバック

: Data from [Data independently produced by Br J Haematol, 2014, 165(1), 89-101]

: , , Mol Cancer Ther, 2017, 16(4):637-648

: ,

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Targeting PI3K inhibitor resistance in breast cancer with metabolic drugs [ Signal Transduct Target Ther, 2025, 10(1):92]	PubMed: 40113784
Tamoxifen induces PI3K activation in uterine cancer [ Nat Genet, 2025, 57(9):2192-2202]	PubMed: 40846762
MicroRNA-mediated PTEN downregulation as a novel non-genetic mechanism of acquired resistance to PI3Kα inhibitors of head & neck squamous cell carcinoma [ Drug Resist Updat, 2025, 81:101251]	PubMed: 40382983
MicroRNA-mediated PTEN downregulation as a novel non-genetic mechanism of acquired resistance to PI3Kα inhibitors of head & neck squamous cell carcinoma [ Drug Resist Updat, 2025, 81:101251]	PubMed: 40382983
Circulating tumor cell plasticity determines breast cancer therapy resistance via neuregulin 1-HER3 signaling [ Nat Cancer, 2025, 6(1):67-85]	PubMed: 39753722
Whole-exome tumor-agnostic ctDNA analysis enhances minimal residual disease detection and reveals relapse mechanisms in localized colon cancer [ Nat Cancer, 2025, 10.1038/s43018-025-00960-z]	PubMed: 40301653
RANKL/PD-1 dual blockade demonstrates survival benefit for patients with advanced lung adenocarcinoma harboring KRAS mutations [ Cell Rep Med, 2025, 6(7):102235]	PubMed: 40669444
Oncogenic PIK3CA corrupts growth factor signaling specificity [ Mol Syst Biol, 2025, 21(2):126-157]	PubMed: 39706867
The SGK3/GSK3β/β-catenin signaling promotes breast cancer stemness and confers resistance to alpelisib therapy [ Int J Biol Sci, 2025, 21(6):2462-2475]	PubMed: 40303291
Role of the PI3K/AKT signaling pathway in the cellular response to Tumor Treating Fields (TTFields) [ Cell Death Dis, 2025, 16(1):210]	PubMed: 40148314

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。