Alpelisib (BYL719)

製品コードS2814 バッチS281407

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)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution

5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O

4.4mg/ml

Taking the 1 mL working solution as an example, add 50 μL 88 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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	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	BYL719(>270 mg/d) shows statistically significant dose-dependent anti-tumor efficacy in PIK3CA mutant xenograft models in rodents. BYL719 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. BYL719(270mg/d) 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 (0–1000 nM) for 72 h. 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

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：

EML4-ALK fusions drive lung adeno-to-squamous transition through JAK-STAT activation [ J Exp Med, 2024, 221(3)e20232028]	PubMed: 38284990
Integrated genomic and transcriptomic analysis reveals the activation of PI3K signaling pathway in HPV-independent cervical cancers [ Br J Cancer, 2024, 10.1038/s41416-023-02555-w]	PubMed: 38253702
Integrative modeling uncovers p21-driven drug resistance and prioritizes therapies for PIK3CA-mutant breast cancer [ NPJ Precis Oncol, 2024, 8(1):20]	PubMed: 38273040
Methyl vinyl ketone and its analogs covalently modify PI3K and alter physiological functions by inhibiting PI3K signaling [ J Biol Chem, 2024, 300(3):105679]	PubMed: 38272219
Evolutionary states and trajectories characterized by distinct pathways stratify patients with ovarian high grade serous carcinoma [ Cancer Cell, 2023, 41(6):1103-1117.e12]	PubMed: 37207655
Generation and multi-dimensional profiling of a childhood cancer cell line atlas defines new therapeutic opportunities [ Cancer Cell, 2023, 41(4):660-677.e7]	PubMed: 37001527
Intact regulation of G1/S transition renders esophageal squamous cell carcinoma sensitive to PI3Kα inhibitors [ Signal Transduct Target Ther, 2023, 8(1):153]	PubMed: 37041169
"Proteotranscriptomic analysis of advanced colorectal cancer patient derived organoids for drug sensitivity prediction" [ J Exp Clin Cancer Res, 2023, 42(1):8]	PubMed: 36604765
Feedback activation of EGFR/wild-type RAS signaling axis limits KRASG12D inhibitor efficacy in KRASG12D-mutated colorectal cancer [ Oncogene, 2023, 42(20):1620-1633]	PubMed: 37020035
Feedback activation of EGFR/wild-type RAS signaling axis limits KRASG12D inhibitor efficacy in KRASG12D-mutated colorectal cancer [ Oncogene, 2023, 10.1038/s41388-023-02676-9 10.3322/caac.21660 10.1001/jama.2021.6021 10.1038/nrdp.2015.65 10.1038/s41575-019-0189-8 10.1038/nature11252 10.1038/s41392]	PubMed: 37020035

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。