Alpelisib (BYL719)

製品コード：S2814 純度：99.96%

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。

CAS No. 1217486-61-7

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
10mg	JPY 35500	国内在庫あり
100mg	JPY 145500	国内在庫あり
1g	JPY 295500	国内在庫あり

代表番号: 045-509-1970\|電子メール：sales@selleck.co.jp よく尋ねられる質問

文献中Selleckの製品使用例（246）

製品安全説明書

現在のバッチを見る：純度： 99.96%

99.96

Alpelisib (BYL719)関連製品

関連ターゲット	p110α p110β p110δ p110γ C2β Vps34	もっと見る
関連製品	LY294002 3-Methyladenine (3-MA) Dactolisib (BEZ235) Pictilisib (GDC-0941) Wortmannin (SL-2052) Buparlisib (BKM120) PI-103 TGX-221 ZSTK474 Omipalisib (GSK2126458) 740 Y-P (PDGFR 740Y-P) Quercetin (Sophoretin) A66 PF-04691502 PIK-75 HCl SAR405 IC-87114 Taselisib (GDC 0032) AS-605240 VPS34-IN1 Apitolisib (GDC-0980) PIK-90 Gedatolisib (PKI-587) Eganelisib (IPI-549) AZD6482 HS-173 AS-252424 AZD8186 GSK2636771 Voxtalisib (XL765) GSK1059615 Samotolisib (LY3023414) VS-5584 (SB2343) Pilaralisib (XL147) CZC24832 TG100-115 BGT226 (NVP-BGT226) maleate XL147 analogue AS-604850 Quercetin Dihydrate GO-203 TFA VPS34 inhibitor 1 (Compound 19) Bimiralisib (PQR309) Paxalisib (GDC-0084) Voxtalisib (XL765) Analogue Serabelisib (TAK-117) GDC-0077 (Inavolisib) PKI-402 AMG319 Nemiralisib SF2523 GNE-317 CH5132799 PIK-294 PI3 Kinase p110β Antibody (Rabbit mAb) [A2M11] TG100713 AZD8835 LY294002 hydrochloride GDC-0326 (E)-Akt inhibitor-IV PI-3065 Selective PI3Kδ Inhibitor 1 (compound 7n) YS-49 GSK2292767 Seletalisib (UCB-5857) leniolisib (CDZ 173) PI3 Kinase p85α Antibody (Mouse mAb) [K4G2] Gallein CAY10505 acalisib (GS-9820) IPI-3063 PI3 Kinase p85 Antibody (Rabbit mAb) [A5E17] PI 3 Kinase p85 β Antibody (Rabbit mAb) [D1J6] PF-4989216 GNE-477 GNE-493	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library PI3K/Akt Inhibitor Library Apoptosis Compound Library Cell Cycle compound library NF-κB Signaling Compound Library	もっと見る

シグナル伝達経路

PI3Kシグナル伝達経路

PI3K阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
H929	Growth Inhibition Assay	0.5-2.5 μM	48 h	inhibits cell growth in a dose-dependent manner	24405121
MM1S	Growth Inhibition Assay	0.5-2.5 μM	48 h	inhibits cell growth in a dose-dependent manner	24405121
MM1R	Growth Inhibition Assay	0.5-2.5 μM	48 h	inhibits cell growth in a dose-dependent manner	24405121
U266	Growth Inhibition Assay	0.5-2.5 μM	48 h	inhibits cell growth in a dose-dependent manner	24405121
OPM1	Growth Inhibition Assay	0.5-2.5 μM	48 h	inhibits cell growth in a dose-dependent manner	24405121
OPM2	Growth Inhibition Assay	0.5-2.5 μM	48 h	inhibits cell growth in a dose-dependent manner	24405121
Mel290	Growth Inhibition Assay	500-2000 nM	5 d	inhibits the phosphorylation of AKT (Ser473) up to 1 μM	24563540
C918	Growth Inhibition Assay	500-2000 nM	5 d	inhibits the phosphorylation of AKT (Ser473) up to 1 μM	24563540
Omm1	Growth Inhibition Assay	500-2000 nM	5 d	inhibits the phosphorylation of AKT (Ser473) up to 1 μM	24563540
Omm1.3	Growth Inhibition Assay	500-2000 nM	5 d	inhibits the phosphorylation of AKT (Ser473) up to 1 μM	24563540
Mel270	Growth Inhibition Assay	500-2000 nM	5 d	inhibits the phosphorylation of AKT (Ser473) up to 1 μM	24563540
92.1	Growth Inhibition Assay	500-2000 nM	5 d	inhibits the phosphorylation of AKT (Ser473) up to 1 μM	24563540
QGP-1	Function Assay	1/10 μM	4 h	inhibits PI3K (AKT Ser308) and mTORC1/2 activities	25026292
BON-1	Function Assay	1/10 μM	4 h	inhibits PI3K (AKT Ser308) and mTORC1/2 activities	25026292
SCC25	Growth Inhibition Assay	0.1-100 μM	72 h	IC50=49.30 μM	25550549
SNU1041	Growth Inhibition Assay	0.1-100 μM	72 h	IC50=20.65 μM	25550549
FaDu	Growth Inhibition Assay	0.1-100 μM	72 h	IC50=19.66 μM	25550549
SNU-1066	Growth Inhibition Assay	0.1-100 μM	72 h	IC50=1.13 μM	25550549
SNU-1076	Growth Inhibition Assay	0.1-100 μM	72 h	IC50=6.82 μM	25550549
Detroit562	Growth Inhibition Assay	0.1-100 μM	72 h	IC50=1.10 μM	25550549
RPMI	Growth Inhibition Assay	0.5-2.5 μM	48 h	inhibits cell growth in a dose-dependent manner	24405121
SKBR3	Growth Inhibition Assay	33 μM	5 d	inhibits 35％ cell growth	23918797
MDA453	Growth Inhibition Assay	33 μM	5 d	inhibits 38％ cell growth	23918797
EFM192A	Growth Inhibition Assay	33 μM	5 d	inhibits 27％ cell growth	23918797
AU565	Growth Inhibition Assay	33 μM	5 d	inhibits 26％ cell growth	23918797
MDA361	Growth Inhibition Assay	33 μM	5 d	inhibits 44％ cell growth	23918797
BT474	Growth Inhibition Assay	33 μM	5 d	inhibits 16％ cell growth	23918797
HCC202	Growth Inhibition Assay	33 μM	5 d	inhibits 20％ cell growth	23918797
KPL4	Growth Inhibition Assay	33 μM	5 d	inhibits 58％ cell growth	23918797
NCL-N87	Growth Inhibition Assay	33 μM	5 d	inhibits 31％ cell growth	23918797
UACC812	Growth Inhibition Assay	33 μM	5 d	inhibits 27％ cell growth	23918797
HCC2218	Growth Inhibition Assay	33 μM	5 d	inhibits 15％ cell growth	23918797
HCC1569	Growth Inhibition Assay	33 μM	5 d	inhibits 5％ cell growth	23918797
OE19	Growth Inhibition Assay	33 μM	5 d	inhibits 23％ cell growth	23918797
OE33	Growth Inhibition Assay	33 μM	5 d	inhibits 23％ cell growth	23918797
JIMT1	Growth Inhibition Assay	33 μM	5 d	inhibits 9％ cell growth	23918797
HCC1954	Growth Inhibition Assay	33 μM	5 d	inhibits 29％ cell growth	23918797
NUGC4	Growth Inhibition Assay	33 μM	5 d	inhibits 14％ cell growth	23918797
ZR-75-30	Growth Inhibition Assay	33 μM	5 d	inhibits -15％ cell growth	23918797
POS-1	Growth Inhibition Assay			IC50=8 μM， IC90=36 μM	24961790
MOS-J	Growth Inhibition Assay			IC50=10 μM， IC90=36 μM	24961790
HOS	Growth Inhibition Assay			IC50=15 μM， IC90=42 μM	24961790
MG-63	Growth Inhibition Assay			IC50=6 μM， IC90=24 μM	24961790
Rat1	P110alpha inhibition assay			IC50 = 0.074 μM	26164189
Rat1	PI3Kalpha inhibition assay			IC50 = 0.074 μM	26206504
Rat1	P110alpha inhibition assay			IC50 = 0.074 μM	23726034
Rat1	P110delta inhibition assay			IC50 = 1.2 μM	26164189
Rat1	PI3Kgamma inhibition assay			IC50 = 1.2 μM	26206504
Rat1	P110delta inhibition assay			IC50 = 1.2 μM	23726034
Rat1	P110beta inhibition assay			IC50 = 2.2 μM	26164189
Rat1	PI3Kbeta inhibition assay			IC50 = 2.2 μM	26206504
Rat1	P110alpha inhibition assay			IC50 = 2.2 μM	23726034
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

Targets

PI3Kα
(Cell-free assay)

5 nM

In Vitro
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.
細胞実験	細胞株	CW2 cells
	濃度	500 nM
	反応時間	72 h
	実験の流れ	Using increasing concentrations of alpelisib (BYL719) (0–1000 nM), cells were treated for 72 h. Cell viability was quantified using the CyQuant assay.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	PIM1 / PIM2 / PIM3 / p-PRAS40 / p-RPS6 / p-BAD pS6 (Ser235-236) p-HER2 / IGF-1R p100β / p110α / p85 / p-ERBB3(Y1289) p-AKT(S473) / p-AKT(T308)		27604488
	Growth inhibition assay	Cell viability		27602501
	Immunofluorescence	LC3		26637440

In Vivo
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 low inter-individual variability in Cmax and AUC in humans. At 270 mg/d, this compound shows first signs of clinical efficacy, including 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.
動物実験	動物モデル	Female athymic nu/nu mice
	投与量	40 mg/kg
	投与経路	o.g.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2026-07-01)
NCT07679269	NOT_YET_RECRUITING	PIK3CA-Related Overgrowth Spectrum (PROS); Breast Neoplasms (Including Advanced or Metastatic Breast Cancer With PIK3CA Mutation)	Novartis Pharmaceuticals	2027-01-01	PHASE2
NCT05933395	RECRUITING	Advanced Breast Cancer	Dartmouth-Hitchcock Medical Center	2024-09-23	PHASE2
NCT05564377	RECRUITING	Advanced Malignant Solid Neoplasm; Anatomic Stage III Breast Cancer AJCC v8; Anatomic Stage IV Breast Cancer AJCC v8; Locally Advanced Malignant Solid Neoplasm; Malignant Female Reproductive System Neoplasm; Metastatic HER2-Negative Breast Carcinoma; Metastatic Malignant Solid Neoplasm; Recurrent Endometrial Carcinoma; Recurrent Fallopian Tube Carcinoma; Recurrent Malignant Female Reproductive System Neoplasm; Recurrent Malignant Solid Neoplasm; Recurrent Ovarian Carcinoma; Recurrent Primary Peritoneal Carcinoma; Unresectable HER2-Negative Breast Carcinoma; Unresectable Malignant Solid Neoplasm	National Cancer Institute (NCI)	2023-04-07	PHASE2
NCT07573696	NOT_YET_RECRUITING	Nonsmall Cell Lung Cancer Stage III	Wen-zhao ZHONG	2026-06-15	PHASE2
NCT07543822	ACTIVE_NOT_RECRUITING	Vascular Anomalies; Vascular Anomaly; TIE2/PIK3CA Pathway Driven Vascular Anomalies	Children's Hospital of Philadelphia	2025-08-27	PHASE2
NCT07778524	RECRUITING	Insulin Resistance; Type 2 Diabetes; Obesity & Overweight; Healthy Adult Participants	Columbia University	2026-09-02	PHASE1

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

参考

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

化学情報

分子量	441.47	化学式	C₁₉H₂₂F₃N₅O₂S
CAS No.	1217486-61-7	SDF	Download Alpelisib (BYL719) SDFをダウンロードする
Smiles	CC1=C(SC(=N1)NC(=O)N2CCCC2C(=O)N)C3=CC(=NC=C3)C(C)(C)C(F)(F)F
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 88 mg/mL ( (199.33 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo Batch: Add solvents to the product individually and in order.				投与溶液組成計算機
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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (11.33mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
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.
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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	4.400mg/ml (9.97mM)	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.
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.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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C1=C0/X	C1:	LOG(C1):
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C6=C5/X	C6:	LOG(C6):
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