Alpelisib | PI3Kα Inhibitor | AmBeed-信号通路专用抑制剂

规格	价格	会员价	库存	数量
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产品名称	C2β ↓ ↑	p110α ↓ ↑	p110β ↓ ↑	p110γ ↓ ↑	p110δ ↓ ↑	PI3K ↓ ↑	Vps34 ↓ ↑	其他靶点	纯度
A66	+ C2β, IC50: 462 nM	++ p110α, IC50: 32 nM							99%+
Taselisib	+ C2β, IC50: 292 nM	++++ PI3Kα, Ki: 0.29 nM	+++ PI3Kβ, Ki: 9.1 nM	++++ PI3Kγ, Ki: 0.97 nM	++++ PI3Kδ, Ki: 0.12 nM		+ hVps34, IC50: 374 nM		99%+
Gedatolisib		++++ PI3Kα, IC50: 0.4 nM		+++ PI3Kγ, IC50: 5.4 nM				mTOR	99%
HS-173		++++ PI3Kα , IC50: 0.8 nM							99%+
Serabelisib		+++ PI3Kα, IC50: 21 nM							99%+
GNE-477		++++ PI3Kα, IC50: 4 nM						mTOR	99%
YM-201636		+ p110α, IC50: 3.3 μM						PIKfyve	98%
AS-252424		+ PI3Kα, IC50: 935 nM		++ PI3Kγ, IC50: 33 nM					99%
Alpelisib		+++ PI3Kα, IC50: 5 nM							99%+
AS-604850		+ PI3Kα, IC50: 4.5 μM		+ PI3Kγ, IC50: 0.25 μM					99%
SF2523		++ PI3Kα, IC50: 34 nM		++ PI3Kγ, IC50: 158 nM				DNA-PK,mTOR	99%+
Inavolisib		++++ PI3K alpha, IC50: 0.038 nM							99%+
Bimiralisib		++++ PI3Kα, Kd: 1.5 nM	+++ PI3Kβ, Kd: 11 nM	++ PI3Kγ, Kd: 25 nM	++ PI3Kδ, Kd: 25 nM			mTOR	99%+
GSK1059615		++++ PI3Kα, IC50: 0.4 nM	++++ PI3Kβ, IC50: 0.6 nM	+++ PI3Kγ, IC50: 5 nM	++++ PI3Kδ, IC50: 2 nM			mTOR	98%
GSK2636771			✔						99%
Fimepinostat		+++ PI3Kα, IC50: 19 nM	++ PI3Kβ, IC50: 54 nM		++ PI3Kδ, IC50: 39 nM				99%+
VS-5584		++++ PI3Kα, IC50: 2.6 nM	+++ PI3Kβ, IC50: 21 nM	++++ PI3Kγ, IC50: 3.0 nM	++++ PI3Kδ, IC50: 2.7 nM			mTOR	98%
Dactolisib		++++ p110α1, IC50: 4 nM	++ p110β, IC50: 75 nM	+++ p110γ, IC50: 5 nM	+++ p110δ, IC50: 7 nM				98+%
PI-103		++++ p110α, IC50: 2 nM	++++ p110β, IC50: 3 nM	+++ p110γ, IC50: 15 nM	++++ p110δ, IC50: 3 nM			DNA-PK,mTOR	99%+
PI-3065			+ p110β, IC50: 1078 nM		+++ p110δ, IC50: 15 nM				99%+
Voxtalisib		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 113 nM	+++ PI3Kγ, IC50: 9 nM	++ PI3Kδ, IC50: 43 nM			DNA-PK,mTOR	99%+
AZD-8835		+++ PI3Kα, IC50: 6.2 nM	+ PI3Kβ, IC50: 431 nM	++ PI3Kγ, IC50: 90 nM	+++ PI3Kδ, IC50: 5.7 nM				99%
Pilaralisib analogue		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 36 nM	+++ PI3Kγ, IC50: 23 nM	++ PI3Kδ, IC50: 36 nM				99%+
ZSTK474		+++ PI3Kα, IC50: 16 nM	++ PI3Kβ, IC50: 44 nM	++ PI3Kγ, IC50: 49 nM	+++ PI3Kδ, IC50: 4.6 nM	++ PI3K, IC50: 37 nM			98%
AS-605240		++ PI3Kα, IC50: 60 nM	+ PI3Kβ, IC50: 270 nM	+++ PI3Kγ, IC50: 8 nM	+ PI3Kδ, IC50: 300 nM				98%
TGX-221			+++ p110β, IC50: 5 nM		++ p110δ, IC50: 0.1 μM				99%+
PF-04691502		++++ PI3Kα, Ki: 1.8 nM	++++ PI3Kβ, Ki: 2.1 nM	++++ PI3Kγ, Ki: 1.9 nM	++++ PI3Kδ, Ki: 1.6 nM			mTOR	98+%
GDC-0084		++++ PI3Kα, Ki app: 2 nM	++ PI3Kβ, Ki app: 46 nM	+++ PI3Kγ, Ki app: 10 nM	++++ PI3Kδ, Ki app: 3 nM			mTOR	99%+
Buparlisib		++ p110α, IC50: 52 nM	+ p110β, IC50: 166 nM	+ p110γ, IC50: 262 nM	++ p110δ, IC50: 116 nM		+ Vps34, IC50: 2.4 μM	mTOR	98%
LY294002		+ p110α, IC50: 0.5 μM	+ p110β, IC50: 0.97 μM		+ p110δ, IC50: 0.57 μM			DNA-PK	99%+
AZD 6482		+ PI3Kα, IC50: 870 nM	+++ PI3Kβ, IC50: 10 nM		++ PI3Kδ, IC50: 80 nM			DNA-PK	99%+
Pictilisib		++++ p110α, IC50: 3 nM	++ p110β, IC50: 33 nM	++ p110γ, IC50: 75 nM	++++ p110δ, IC50: 3 nM			mTOR	99%+
PKI-402		++++ PI3Kα, IC50: 2 nM	+++ PI3Kβ, IC50: 7 nM	+++ PI3Kγ, IC50: 16 nM	+++ PI3Kδ, IC50: 14 nM			mTOR	98%
Copanlisib		++++ PI3Kα, IC50: 0.5 nM	++++ PI3Kβ, IC50: 3.7 nM	+++ PI3Kγ, IC50: 6.4 nM	++++ PI3Kδ, IC50: 0.7 nM				99%+
Omipalisib		++++ p110α, Ki: 0.019 nM	++++ p110β, Ki: 0.13 nM	++++ p110γ, Ki: 0.06 nM	++++ p110δ, Ki: 0.024 nM				99%+
Izorlisib		+++ PI3Kα, IC50: 14 nM	++ PI3Kβ, IC50: 0.12 μM	++ PI3Kγ, IC50: 36 nM	+ PI3Kδ, IC50: 0.50 μM				99%+
AZD8186		++ PI3Kα, IC50: 35 nM	++++ PI3Kβ, IC50: 4 nM		+++ PI3Kδ, IC50: 12 nM				99%
KU-0060648		++++ PI3Kα, IC50: 4 nM	++++ PI3Kβ, IC50: 0.5 nM	+ PI3Kγ, IC50: 0.59 μM	++++ PI3Kδ, IC50: 0.1 nM			DNA-PK	98%
Apitolisib		+++ p110α, IC50: 5 nM	++ p110β, IC50: 27 nM	+++ p110γ, IC50: 14 nM	+++ p110δ, IC50: 7 nM			mTOR	98%+
CZC24832			+ PI3Kβ, IC50: 1.1 μM	++ PI3Kγ, IC50: 27 nM					98+%
BGT226 maleate		++++ PI3Kα, IC50: 4 nM	++ PI3Kβ, IC50: 63 nM	++ PI3Kγ, IC50: 38 nM				mTOR	99%+
TG 100713		++ PI3Kα, IC50: 165 nM	+ PI3Kβ, IC50: 215 nM	++ PI3Kγ, IC50: 50 nM	+++ PI3Kδ, IC50: 24 nM				98%+
PI3K-IN-1		++ PI3Kα, IC50: 39 nM	++ PI3Kβ, IC50: 113 nM	+++ PI3Kγ, IC50: 9 nM	++ PI3Kδ, IC50: 43 nM			DNA-PK,mTOR	98+%
TG100-115		+ PI3Kα, IC50: 1.3 μM	+ PI3Kβ, IC50: 1.2 μM	++ PI3Kγ, IC50: 83 nM	+ PI3Kδ, IC50: 235 nM				98%
PIK-90		+++ PI3Kα, IC50: 11 nM	+ PI3Kβ, IC50: 350 nM	+++ PI3Kγ, IC50: 18 nM	++ PI3Kδ, IC50: 58 nM				99%+
PIK-294			+ p110β, IC50: 490 nM	++ p110γ, IC50: 160 nM	+++ p110δ, IC50: 10 nM				99%+
Duvelisib			++++ PI3Kβ, Ki: 1564 pM	++ PI3Kγ, Ki: 243 pM	++++ PI3Kδ, Ki: 23 pM				99%+
GDC-0326		++++ PI3Kα, Ki: 0.2 nM	++ PI3Kβ, Ki: 26.6 nM	+++ PI3Kγ, Ki: 10.2 nM	++++ PI3Kδ, Ki: 4 nM				98%
Quercetin Dihydrate			+ PI3Kβ, IC50: 5.4 μM	+ PI3Kγ, IC50: 2.4 μM	+ PI3Kδ, IC50: 3.0 μM				95%
Quercetin			+ PI3Kβ, IC50: 5.4 μM	+ PI3Kγ, IC50: 2.4 μM	+ PI3Kδ, IC50: 3.0 μM			Sirtuin,PKC,Src	95%
Leniolisib		+ PI3Kα, IC50: 0.244 μM	+ PI3Kβ, IC50: 0.424 μM	+ PI3Kγ, IC50: 2.23 μM	+++ PI3Kδ, IC50: 0.011 μM			DNA-PK	99%+
PIK-108			✔						99%
Eganelisib				+++ PI3Kγ, IC50: 16 nM					99%+
CAY10505				✔					99%
IPI-3063					++++ p110δ, IC50: 2.5 nM				99%
Nemiralisib					++++ PI3Kδ, pKi: 9.9				99%+
PF-4989216		++++ p110α, IC50: 2 nM		++ p110γ, IC50: 65 nM	++++ p110δ, IC50: 1 nM				99%+
PIK-75 HCl		+++ p110α, IC50: 5.8 nM		++ p110γ, IC50: 76 nM	+ p110δ, IC50: 0.51 μM			DNA-PK	99%+
Tenalisib				++ PI3Kγ, IC50: 33.2 nM	++ PI3Kδ, IC50: 24.5 nM				98%
Acalisib					+++ p110δ, IC50: 14 nM				99%+
Umbralisib					+++ PI3Kδ, IC50: 22.2 nM				99%+
AMG319				+ PI3Kγ, IC50: 850 nM	+++ PI3Kδ, IC50: 18 nM				99%
IC-87114				+ PI3Kγ, IC50: 29 μM	+ PI3Kδ, IC50: 0.5 μM				99%+
Idelalisib				++ p110γ, IC50: 89 nM	++++ p110δ, IC50: 2.5 nM				98%
PIK-293				+ p110γ, IC50: 10 μM	+ p110δ, IC50: 0.24 μM				99%+
Vps34-PIK-III					+ PI3Kδ, IC50: 1.2μM		+++ Vps34, IC50: 0.018μM		99%+
GSK2292767					✔				98%
Seletalisib				+ PI3Kγ, IC50: 282 nM	+++ PI3Kδ, IC50: 12 nM				99%+
P110δ-IN-1					++++ P110δ, IC50: 0.6 nM				99%
PI3Kδ-IN-5					++++ PI3Kδ, IC50: 0.9 nM				99%
SRX3207		+ PI3K alpha, IC50: 244 nM		+ PI3K gamma, IC50: 9790 nM	+ PI3K delta, IC50: 388 nM			Syk	98%
Parsaclisib HCl					++++ PI3Kδ, IC50: 1 nM				98%
IHMT-PI3Kδ-372					+++ PI3Kδ, IC50: 14 nM				98%
Trigonelline						✔		Akt	99%+
Wortmannin						++++ PI3K, IC50: 3 nM		DNA-PK,MLCK	99%+
Samotolisib						✔		DNA-PK	99%+
GNE-317						✔			99%+
Oroxin B						✔		Akt,PTEN	99%+
NU 7026						+ PI3K, IC50: 13 μM		DNA-PK	98+%
Deguelin						✔		Akt	99%+
Ailanthone						✔		CDK,Akt,ATM/ATR	98%
Resibufogenin						✔		ROS	98%
KU-57788						+ PI3K, IC50: 5 μM		DNA-PK,mTOR	99%+
Cinobufagine						✔		Akt	99%
α-Linolenic acid						✔			97% (GC)
MTX-211						✔		EGFR	98%
PI3K/mTOR Inhibitor-2						++++ PI3K, IC50: 3.4 nM		mTOR	99%+
SPP-86						✔			99%+
(E)-Akt inhibitor-IV						✔			98%
Vps34-IN-1							++ Vps34, IC50: 25 nM		98%
SAR405							++++ Vps34, IC50: 1.2 nM		98+%
3-Methyladenine				+ PI3Kγ, IC50: 60 μM			+ Vps34, IC50: 25 μM	Autophagy	98%
Vps34-IN-4							+++ VPS34, IC50: 15 nM		98%+
Autophinib							+++ Vps34, IC50: 19 nM	Autophagy	99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Cell Line MCF7 T47D OVCAR3 ovarian cancer cells SKOV3 ovarian cancer cells HK2 cells HEK293T cells CAL-33 MCF7 cells T47D cells MCF7 MAGI1 KO cells MCF7 MAGI1 KO cells OcrlY/- mouse PTCs	Concentration	Treated Time	Description	References
MCF7	0.1 µM	6 days	To validate the effect of combining PI3K α inhibitor alpelisib with MCL1 inhibitor s63845, the results showed that the combination was more efficacious than each drug alone and induced more apoptosis	Cancer Res. 2021 Sep 1;81(17):4603-4617.
T47D	0.1 µM	6 days	To validate the effect of combining PI3K α inhibitor alpelisib with MCL1 inhibitor s63845 and BCL-2/BCL-XL inhibitor navitoclax, the results showed that the combination was more efficacious than each drug alone and induced more apoptosis	Cancer Res. 2021 Sep 1;81(17):4603-4617.
OVCAR3 ovarian cancer cells	5 μM	1–4 days	To evaluate the effect of insulin on the antiproliferative effects of PI3Ki. Results showed that insulin significantly reversed the inhibitory effect of BYL719 on p-AKT and attenuated the antiproliferative effects of PI3Ki.	Mol Metab. 2025 Jun;96:102151
SKOV3 ovarian cancer cells	5 μM	1–4 days	To evaluate the effect of insulin on the antiproliferative effects of PI3Ki. Results showed that insulin significantly reversed the inhibitory effect of BYL719 on p-AKT and attenuated the antiproliferative effects of PI3Ki.	Mol Metab. 2025 Jun;96:102151
HK2 cells	10 µM	16 h	Reduced aberrant actin polymerization, improved endocytic defect	Kidney Int. 2020 Oct;98(4):883-896.
HEK293T cells	1 μM	24 h	To identify the methyltransferase responsible for methylating K1330 of KMT2D	Cell Rep. 2024 May 28;43(5):114174.
CAL-33	0.5 μM	30 min	To study the effect of Alpelisib on the PI3K signaling pathway, results showed that Alpelisib inhibited the PI3K signaling pathway	Science. 2021 Oct;374(6563):eabf3067.
MCF7 cells	250 nM	48 h	To investigate the effect of Alpelisib on cell cycle proteins, results showed inhibitory effect in MCF7 cells	Oncogene. 2022 Jul;41(27):3524-3538.
T47D cells	250 nM	48 h	To investigate the effect of Alpelisib on cell cycle proteins, results showed stronger inhibitory effect in T47D cells	Oncogene. 2022 Jul;41(27):3524-3538.
MCF7 MAGI1 KO cells	2 µM	72 h	To investigate the effect of Alpelisib on the activation of DNA repair proteins in MCF7 MAGI1 KO cells, results showed that DNA repair proteins (e.g., DNA-PKs, phospho-ATM (S1981), phospho-p95/NSB1 (S343), and XLF) were upregulated after Alpelisib treatment.	Cells. 2023 Jul 25;12(15):1929.
MCF7 MAGI1 KO cells	2 µM	72 h	To study the effect of Alpelisib in combination with Fulvestrant on MCF7 MAGI1 KO cells, results showed that the combination treatment significantly reduced cell viability.	Cells. 2023 Jul 25;12(15):1929.
OcrlY/- mouse PTCs	10 µM	16 h	Restored stress fiber architecture, reduced endosomal actin staining	Kidney Int. 2020 Oct;98(4):883-896.

Species Mice Mice Mice Mouse Mice Nude mice	Animal Model Orthotopic mammary allograft tumour model MCF7 human breast cancer xenograft model MCF7 xenograft models OcrlY/- mouse model Orthotopic osteosarcoma model Xenograft tumor model	Administration	Dosage	Frequency	Description	References
Mice	Orthotopic mammary allograft tumour model	Oral	45 mg/kg	Once per day for 10 days	Investigate the effect of PI3K signaling on PANK4 phosphorylation, results showed PI3K inhibition diminished PANK4 phosphorylation	Nature. 2022 Aug;608(7921):192-198
Mice	MCF7 human breast cancer xenograft model	Oral	25 mg/kg	Once daily for the indicated times	To evaluate the antitumor activity of SMYD2 knockdown combined with Alpelisib	Cell Rep. 2024 May 28;43(5):114174.
Mice	MCF7 xenograft models	Oral	125 nM	6 days a week for 3 weeks	To investigate the inhibitory effect of Alpelisib on tumor growth in vivo, results showed partial inhibition in RB-deficient tumors	Oncogene. 2022 Jul;41(27):3524-3538.
Mouse	OcrlY/- mouse model	Oral gavage	50 mg/kg	Daily for 6 weeks	Reduced endosomal actin staining, improved endocytic function, reduced proteinuria	Kidney Int. 2020 Oct;98(4):883-896.
Mice	Orthotopic osteosarcoma model	Oral	50 mg/kg	Daily for 7 days	Evaluate the anti-tumor effect of Alpelisib in the mouse orthotopic osteosarcoma model, results showed that Alpelisib significantly inhibited tumor growth	Adv Healthc Mater. 2022 Sep;11(17):e2200768
Nude mice	Xenograft tumor model	Oral	12.5 mg/kg	Once daily	The combination of Alpelisib and EZH inhibitor Tazemetostat induces regression of xenograft tumors harboring a PIK3CA helical domain mutation, but not tumors with either a WT PIK3CA or a PIK3CA kinase domain mutation.	Nat Commun. 2022 Apr 13;13(1):1974

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT02167854	Breast Cancer	Phase 1	Active, not recruiting	June 2019	United States, New Jersey ... 展开 >> Memorial Sloan Kettering at Basking Ridge Basking Ridge, New Jersey, United States, 07920 Memorial Sloan Kettering Monmouth Middletown, New Jersey, United States, 07748 United States, New York Memorial Sloan Kettering Commack Commack, New York, United States, 11725 Memoral Sloan Kettering Westchester Harrison, New York, United States, 10604 Memorial Sloan Kettering Cancer Center New York, New York, United States, 10065 Memorial Sloan Kettering Rockville Centre Rockville Centre, New York, United States, 11570 收起 <<
NCT02734615	Advanced or Metastatic ER+ Bre... 展开 >>ast Cancer 收起 <<	Phase 1	Recruiting	October 30, 2020	United States, Maryland ... 展开 >> Novartis Investigative Site Recruiting Baltimore, Maryland, United States, 21287 United States, Massachusetts Massachusetts General Hospital Massachusetts General Hospital Recruiting Boston, Massachusetts, United States, 02114 Contact: Dejan Juric, MD 617-726-6500 Juric.Dejan@mgh.harvard.edu Contact: Meghan Miles 617-726-6500 MEMILES@mgh.harvard.edu Principal Investigator: Dejan Juric, MD United States, New York Novartis Investigative Site Recruiting New York, New York, United States, 10021 Contact: Alexandra Burleigh 646-422-4394 burleiga@mskcc.org Principal Investigator: Komal Jhaveri United States, Texas Novartis Investigative Site Recruiting Houston, Texas, United States, 77030 Contact: Daniela Westerhold diwesterhold@mdanderson.org Principal Investigator: Rachel M Layman Belgium Novartis Investigative Site Recruiting Bruxelles, Belgium, 1200 Canada, Ontario Novartis Investigative Site Recruiting Toronto, Ontario, Canada, M5G 2M9 France Novartis Investigative Site Recruiting Lyon Cedex, France, 69373 Italy Novartis Investigative Site Recruiting Milano, MI, Italy, 20133 Novartis Investigative Site Recruiting Milano, MI, Italy, 20141 Japan Novartis Investigative Site Recruiting Koto-ku, Tokyo, Japan, 135 8550 Singapore Novartis Investigative Site Recruiting Singapore, Singapore, 169610 Spain Novartis Investigative Site Recruiting Barcelona, Catalunya, Spain, 08036 Novartis Investigative Site Recruiting Madrid, Spain, 28007 收起 <<
NCT03138070	Head and Neck Squamous Cell Ca... 展开 >>ncer 收起 <<	Not Applicable	Recruiting	May 2020	Canada, Ontario ... 展开 >> London Health Sciences Centre, London Regional Cancer Program Recruiting London, Ontario, Canada, N6A 4L6 Contact: Anthony Nichols 519-685-8500 ext 58804 anthony.nichols@lhsc.on.ca Contact: Shamim Mortuza 519-685-8500 ext 58618 shamim.mortuza@lhsc.on.ca 收起 <<
NCT01602315	Recurrent Head and Neck Squamo... 展开 >>us Cell Carcinoma Metastatic Head and Neck Squamous Cell Carcinoma 收起 <<	Phase 1 Phase 2	Terminated(early termination d... 展开 >>ue to Sponsor decision (slow recruitment)) 收起 <<	-	-
NCT01708161	PIK3CA Mutated Advanced Solid ... 展开 >>Tumors PIK3CA Amplified Advanced Solid Tumors 收起 <<	Phase 1 Phase 2	Terminated	-	United States, California ... 展开 >> Novartis Investigative Site Los Angeles, California, United States, 90095 United States, Massachusetts Novartis Investigative Site Boston, Massachusetts, United States, 02114 United States, New York Novartis Investigative Site New York, New York, United States, 10017 United States, Tennessee Novartis Investigative Site Nashville, Tennessee, United States, 37203 Belgium Novartis Investigative Site Leuven, Belgium, 3000 Canada, Ontario Novartis Investigative Site Toronto, Ontario, Canada, M5G 1Z6 Spain Novartis Investigative Site Sevilla, Andalucia, Spain, 41013 Novartis Investigative Site Barcelona, Catalunya, Spain, 08035 Novartis Investigative Site Madrid, Spain, 28033 Novartis Investigative Site Madrid, Spain, 28041 收起 <<
NCT01923168	Breast Cancer	Phase 2	Completed	-	-
NCT01923168	-		Completed	-	-
NCT01602315	-		Terminated(early termination d... 展开 >>ue to Sponsor decision (slow recruitment)) 收起 <<	-	-
NCT03706573	-		-	-	-
NCT01708161	-		Terminated	-	-
NCT03056755	Breast Cancer	Phase 2	Recruiting	April 10, 2020	-
NCT03601507	CDKN2A-p16 Positive ... 展开 >> Human Papillomavirus Positive Oropharyngeal Squamous Cell Carcinoma Stage I Oropharyngeal Squamous Cell Carcinoma AJCC v6 and v7 Stage II Oropharyngeal Squamous Cell Carcinoma AJCC v6 and v7 Stage III Oropharyngeal Squamous Cell Carcinoma AJCC v7 Stage IVA Oropharyngeal Squamous Cell Carcinoma AJCC v7 收起 <<	Phase 2	Recruiting	December 31, 2022	United States, Arizona ... 展开 >> The University of Arizona Medical Center-University Campus Recruiting Tucson, Arizona, United States, 85724 Contact: Julie E. Bauman 520-626-4101 jebauman@email.arizona.edu Principal Investigator: Julie E. Bauman 收起 <<
NCT02624557	Hepatic Impairment	Phase 1	Completed	-	United States, Colorado ... 展开 >> DaVita Clinical Research-Denver Lakewood, Colorado, United States, 80228 United States, Florida University of Miami / Clinical Research Services, Inc. Miami, Florida, United States, 33136 Orlando Clinical Research Center Orlando, Florida, United States, 32809 United States, Minnesota DaVita Clinical Research Minneapolis, Minnesota, United States, 55404 收起 <<
NCT02058381	Pre-menopausal Breast Cancer ... 展开 >> PI3K Pathway Inhibition 收起 <<	Phase 1	Completed	-	Hong Kong ... 展开 >> Novartis Investigative Site Hong Kong, Hong Kong Korea, Republic of Novartis Investigative Site Seongnam-si, Gyeonggi-do, Korea, Republic of, 13620 Novartis Investigative Site Gyeonggi-do, Korea, Korea, Republic of, 10408 Novartis Investigative Site Seoul, Korea, Korea, Republic of, 05505 Novartis Investigative Site Seoul, Korea, Korea, Republic of, 06351 Novartis Investigative Site Seoul, Korea, Republic of, 03722 Taiwan Novartis Investigative Site Kuei-Shan Chiang, Taoyuan/ Taiwan ROC, Taiwan, 33305 Novartis Investigative Site New Taipei City, TWN, Taiwan, 23561 Novartis Investigative Site Kaohsiung City, Taiwan, 83301 Novartis Investigative Site Taichung, Taiwan, 407 Novartis Investigative Site Taipei, Taiwan, 10002 Novartis Investigative Site Taipei, Taiwan, 10449 Novartis Investigative Site Taipei, Taiwan, 112 Thailand Novartis Investigative Site Bangkok, Thailand, 10330 Novartis Investigative Site Chiang Mai, Thailand, 50200 收起 <<
NCT02437318	Breast Cancer	Phase 3	Active, not recruiting	April 15, 2020	-
NCT03631953	Meningioma	Phase 1	Not yet recruiting	January 1, 2022	France ... 展开 >> Assistance Publique Hôpitaux de Marseille Not yet recruiting Marseille, France, 13354 Contact: Thomas GRAILLON, PH 491385545 ext +33 thomas.graillon@ap-hm.fr Contact: Olivier CHINOT, PU-PH 491385545 ext +33 olivier.chinot@ap-hm.fr Principal Investigator: Thomas GRAILLON, PH 收起 <<
NCT03207529	Malignant Neoplasm of Breast	Phase 1	Not yet recruiting	January 2021	United States, Texas ... 展开 >> University of Texas MD Anderson Cancer Center Not yet recruiting Houston, Texas, United States, 77030 Contact: Clinical Research Operations mskaruturi@mdanderson.org 收起 <<
NCT02077933	Neoplasms Bre... 展开 >>ast Neoplasms Kidney Neoplasms Pancreatic Neuroendocine Neoplasms 收起 <<	Phase 1	Active, not recruiting	November 30, 2018	United States, Arkansas ... 展开 >> Highlands Oncology Group Fayetteville, Arkansas, United States, 72703 United States, New York Memorial Sloan Kettering Cancer Center SC - BYL719Z2102 New York, New York, United States, 10065 France Novartis Investigative Site Bordeaux Cedex, France, 33075 Novartis Investigative Site Bordeaux, France, 33076 Novartis Investigative Site Villejuif Cedex, France, 94805 Germany Novartis Investigative Site Berlin, Germany, 12203 Novartis Investigative Site Essen, Germany, 45136 Novartis Investigative Site Essen, Germany, 45147 Novartis Investigative Site Hannover, Germany, 30625 Hong Kong Novartis Investigative Site Hong Kong, Hong Kong Hungary Novartis Investigative Site Budapest, Hungary, H-1077 Italy Novartis Investigative Site Ancona, AN, Italy, 60126 Novartis Investigative Site Milano, MI, Italy, 20141 Novartis Investigative Site Modena, MO, Italy, 41124 Novartis Investigative Site Verona, VR, Italy, 37126 Netherlands Novartis Investigative Site Amsterdam, Netherlands, 1066 CX Novartis Investigative Site Utrecht, Netherlands, 3584CX Spain Novartis Investigative Site Barcelona, Catalunya, Spain, 08036 Novartis Investigative Site Madrid, Spain, 28007 Novartis Investigative Site Madrid, Spain, 28034 United Kingdom Novartis Investigative Site Manchester, United Kingdom, M20 4BX 收起 <<
NCT03386162	Breast Cancer, PI3K, Alpelisib	Phase 2	Recruiting	July 1, 2023	France ... 展开 >> Institut de Cancérologie de l'Ouest/Paul Papin Recruiting Angers, France Contact: Mario CAMPONE, MD, PhD mario.campone@ico.unicancer.fr Principal Investigator: Mario CAMPONE, MD, PhD Institut Sainte-Catherine Recruiting Avignon, France Contact: Alice Mege, MD Principal Investigator: Alice Mege, MD Institut Bergonié Recruiting Bordeaux, France Contact: Marc DEBLED, MD Principal Investigator: Marc DEBLED, MD Polyclinique Bordeaux Nord Aquitaine Recruiting Bordeaux, France Contact: Nadine DOHOLLOU, MD Centre François Baclesse Recruiting Caen, France Contact: Christelle Levy Principal Investigator: Christelle Levy, MD Centre Jean Perrin Recruiting Clermont-ferrand, France, 63011 Contact: Marie-Ange MOURET-REYNIER Principal Investigator: Marie Ange MOURET-REYNIER CH Alpes Leman Recruiting Contamine-sur-Arve, France Contact: Carol ALLIOT, MD Centre de Lutte Contre le Cancer Georges-Francois Leclerc Recruiting Dijon, France, 21079 Contact: Nicolas Isambert, MD 33-3-8073-7506 Chd Vendee Recruiting La Roche Sur Yon, France Contact: Tifenn L'HARIDON, MD Principal Investigator: Tifenn L'HARIDON, MD Centre Oscar Lambret Recruiting Lille, France Contact: Nuria KOTECKI, MD Principal Investigator: Nuria KOTECKI, MD CHU Dupuytren Recruiting Limoges, France Contact: Laurence VENAT-BOUVET, MD Centre Hospitalier Lyon Sud Recruiting Lyon, France Contact: Benoit You, MD Principal Investigator: Benoit You, MD Centre Leon Berard Recruiting Lyon, France Contact: Thomas BACHELOT, MD Principal Investigator: Thomas BACHELOT, MD Hôpital Privé Jean Mermoz Recruiting Lyon, France Contact: Olfa DERBEL, MD Institut Paoli Calmettes Recruiting Marseille, France Contact: Anthony Gonçalves, MD, PhD Principal Investigator: Anthony Gonçalves, MD, PhD CInstitut Regional du cancer-Centre Val D'Aurelle Recruiting Montpellier, France Contact: William JACOT, MD Principal Investigator: William JACOT, MD Centre Alexis Vautrin Recruiting Nancy, France Contact: Vicent Massard Principal Investigator: Vincent Massard, MD Institut de Cancérologie de l'Ouest/ René Gauducheau Recruiting Nantes, France Contact: Mario Campone, MD, PhD Principal Investigator: Mario Campone, MD, PhD Centre Antoine Lacassagne Recruiting Nice, France Contact: Jean-Marc Ferrero Principal Investigator: Jean-Marc Ferrero, MD Institut Curie Recruiting Paris, France Contact: Marie-Paule Sablin, MD mariepaule.sablin@curie.fr Principal Investigator: Marie-Paule Sablin, MD Centre Eugène Marquis Recruiting Rennes, France Contact: Claudia Lefeuvre Plesse Principal Investigator: Claudia Lefeuvre Plesse, MD Centre Henri Becquerel Recruiting Rouen, France Contact: Jean-Christophe Théry, MD Principal Investigator: Jean-Christophe Théry, MD Centre Rene Huguenin Recruiting Saint Cloud, France, 92211 Contact: Florence COUSSY, MD Chru Strasbourg - Nouvel Hopital Civil Recruiting Strasbourg, France Contact: Philippe BARTHELEMY, MD Principal Investigator: Philippe BARTHELEMY, MD Hôpitaux du Léman Recruiting Thonon-les-bains, France, 74200 Contact: Francesco DEL PIANO Principal Investigator: Francesco DEL PIANO CHI de Toulon - Hôpital Sainte-Musse Recruiting Toulon, France Contact: Xavier TCHIKNAVORIAN, MD Principal Investigator: Xavier TCHIKNAVORIAN, MD Institut Claudius Regaud Recruiting Toulouse, France Contact: Florence Dalenc, MD Principal Investigator: Florence Dalenc, MD Institut Gustave Roussy Recruiting Villejuif, France Contact: Monica ARNEDOS, MD Principal Investigator: Monica ARNEDOS, MD 收起 <<
NCT02620839	Solid Tumors	Phase 1	Recruiting	March 2020	United States, California ... 展开 >> UCSF Helen Diller Family Comprehensive Cancer Center Recruiting San Francisco, California, United States, 94143-1711 Contact: Pamela N. Munster, MD 877-827-3222 cancertrials@ucsf.edu 收起 <<

靶点	p110α PI3Kα, IC50:5 nM
描述	There three kinds of catalytic subunits of Class IA PI3Ks, p110α, p110β and p110δ. One of the subunits, P110α, is encoded by PIK3CA in human, which is found to be mutated in many human cancers, for example, colorectal cancers, glioblastomas, gastric cancers, hepatocellular carcinomas, breast cancers. Alpelisib, also called as BYL719, is an orally available p110α inhibitor against with IC50 of 5 nM, less potent to p110β (IC50 = 1.2 μM), p110γ (IC50 = 0.25 μM) and PI3Kδ (IC50 = 0.29 μM, measured by biochemical assay). Alpelisib can block the PI3K/Akt signaling pathway resulting in inhibition of Akt phosphorylation in Rat1-myr-p110x cells^[1]. Alpelisib exhibits potent anti-proliferative and anti-tumor activities in lung squamous cell carcinoma (LSCC) in a PIK3CA-dependent manner^[2]. Now Alpelisib is used in phase I/II trials in patients with breast cancer, lung cancer, pancreatic cancer and squamous cell carcinoma etc.^[3].
作用机制	Alpelisib can interact with the ATP binding pocket of p110α^[1].

CAS号	1217486-61-7
分子式	C₁₉H₂₂F₃N₅O₂S
分子量	441.47
SMILES Code	O=C(N1[C@H](C(N)=O)CCC1)NC2=NC(C)=C(C3=CC(C(C)(C)C(F)(F)F)=NC=C3)S2
MDL No.	MFCD22417085

别名	BYL-719; NVP-BYL719
运输	蓝冰
InChI Key	STUWGJZDJHPWGZ-LBPRGKRZSA-N
Pubchem ID	56649450

92.1	500-2000 nM	Growth Inhibition Assay	5 d	inhibits the phosphorylation of AKT (Ser473) up to 1 μM	24563540
AU565	33 μM	Growth Inhibition Assay	5 d	inhibits 26％ cell growth	23918797
BON-1	1/10 μM	Function Assay	4 h	inhibits PI3K (AKT Ser308) and mTORC1/2 activities	25026292
BT474	33 μM	Growth Inhibition Assay	5 d	inhibits 16％ cell growth	23918797
C918	500-2000 nM	Growth Inhibition Assay	5 d	inhibits the phosphorylation of AKT (Ser473) up to 1 μM	24563540
Detroit562	0.1-100 μM	Growth Inhibition Assay	72 h	IC50=1.10 μM	25550549
EFM192A	33 μM	Growth Inhibition Assay	5 d	inhibits 27％ cell growth	23918797
FaDu	0.1-100 μM	Growth Inhibition Assay	72 h	IC50=19.66 μM	25550549
H929	0.5-2.5 μM	Growth Inhibition Assay	48 h	inhibits cell growth in a dose-dependent manner	24405121
HCC1569	33 μM	Growth Inhibition Assay	5 d	inhibits 5％ cell growth	23918797
HCC1954	33 μM	Growth Inhibition Assay	5 d	inhibits 29％ cell growth	23918797
HCC202	33 μM	Growth Inhibition Assay	5 d	inhibits 20％ cell growth	23918797
HCC2218	33 μM	Growth Inhibition Assay	5 d	inhibits 15％ cell growth	23918797
HOS		Growth Inhibition Assay		IC50=15 μM， IC90=42 μM	24961790
JIMT1	33 μM	Growth Inhibition Assay	5 d	inhibits 9％ cell growth	23918797
KPL4	33 μM	Growth Inhibition Assay	5 d	inhibits 58％ cell growth	23918797
MDA361	33 μM	Growth Inhibition Assay	5 d	inhibits 44％ cell growth	23918797
MDA453	33 μM	Growth Inhibition Assay	5 d	inhibits 38％ cell growth	23918797
Mel270	500-2000 nM	Growth Inhibition Assay	5 d	inhibits the phosphorylation of AKT (Ser473) up to 1 μM	24563540
Mel290	500-2000 nM	Growth Inhibition Assay	5 d	inhibits the phosphorylation of AKT (Ser473) up to 1 μM	24563540
MG-63		Growth Inhibition Assay		IC50=6 μM， IC90=24 μM	24961790
MM1R	0.5-2.5 μM	Growth Inhibition Assay	48 h	inhibits cell growth in a dose-dependent manner	24405121
MM1S	0.5-2.5 μM	Growth Inhibition Assay	48 h	inhibits cell growth in a dose-dependent manner	24405121
MOS-J		Growth Inhibition Assay		IC50=10 μM， IC90=36 μM	24961790
NCL-N87	33 μM	Growth Inhibition Assay	5 d	inhibits 31％ cell growth	23918797
NUGC4	33 μM	Growth Inhibition Assay	5 d	inhibits 14％ cell growth	23918797
OE19	33 μM	Growth Inhibition Assay	5 d	inhibits 23％ cell growth	23918797
OE33	33 μM	Growth Inhibition Assay	5 d	inhibits 23％ cell growth	23918797
Omm1	500-2000 nM	Growth Inhibition Assay	5 d	inhibits the phosphorylation of AKT (Ser473) up to 1 μM	24563540
Omm1.3	500-2000 nM	Growth Inhibition Assay	5 d	inhibits the phosphorylation of AKT (Ser473) up to 1 μM	24563540
OPM1	0.5-2.5 μM	Growth Inhibition Assay	48 h	inhibits cell growth in a dose-dependent manner	24405121
OPM2	0.5-2.5 μM	Growth Inhibition Assay	48 h	inhibits cell growth in a dose-dependent manner	24405121
POS-1		Growth Inhibition Assay		IC50=8 μM， IC90=36 μM	24961790
QGP-1	1/10 μM	Function Assay	4 h	inhibits PI3K (AKT Ser308) and mTORC1/2 activities	25026292
RPMI	0.5-2.5 μM	Growth Inhibition Assay	48 h	inhibits cell growth in a dose-dependent manner	24405121
SCC25	0.1-100 μM	Growth Inhibition Assay	72 h	IC50=49.30 μM	25550549
SKBR3	33 μM	Growth Inhibition Assay	5 d	inhibits 35％ cell growth	23918797
SNU1041	0.1-100 μM	Growth Inhibition Assay	72 h	IC50=20.65 μM	25550549
SNU-1066	0.1-100 μM	Growth Inhibition Assay	72 h	IC50=1.13 μM	25550549
SNU-1076	0.1-100 μM	Growth Inhibition Assay	72 h	IC50=6.82 μM	25550549
U266	0.5-2.5 μM	Growth Inhibition Assay	48 h	inhibits cell growth in a dose-dependent manner	24405121
UACC812	33 μM	Growth Inhibition Assay	5 d	inhibits 27％ cell growth	23918797
ZR-75-30	33 μM	Growth Inhibition Assay	5 d	inhibits -15％ cell growth	23918797

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