Home PI3K/Akt/mTOR PI3K inhibitor Alpelisib (BYL719)

연구용

Alpelisib (BYL719) PI3Kα inhibitor

제품 번호: S2814

Alpelisib (BYL719) is a potent and selective PI3Kα inhibitor with IC50 of 5 nM in a cell-free assay, and minimal effect on PI3Kβ/γ/δ. This compound is in Phase 2.
Alpelisib (BYL719) PI3K inhibitor Chemical Structure

화학 구조

분자량: 441.47

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품질 관리 (Quality Control)

배치: 순도: 99.96%
99.96

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
Detroit562 Growth Inhibition Assay 0.1-100 μM 72 h IC50=1.10 μM 25550549
SNU-1076 Growth Inhibition Assay 0.1-100 μM 72 h IC50=6.82 μM 25550549
SNU-1066 Growth Inhibition Assay 0.1-100 μM 72 h IC50=1.13 μM 25550549
FaDu Growth Inhibition Assay 0.1-100 μM 72 h IC50=19.66 μM 25550549
SNU1041 Growth Inhibition Assay 0.1-100 μM 72 h IC50=20.65 μM 25550549
SCC25 Growth Inhibition Assay 0.1-100 μM 72 h IC50=49.30 μM 25550549
BON-1 Function Assay 1/10 μM 4 h inhibits PI3K (AKT Ser308) and mTORC1/2 activities 25026292
QGP-1 Function Assay 1/10 μM 4 h inhibits PI3K (AKT Ser308) and mTORC1/2 activities 25026292
MG-63 Growth Inhibition Assay IC50=6 μM， IC90=24 μM 24961790
HOS Growth Inhibition Assay IC50=15 μM， IC90=42 μM 24961790
MOS-J Growth Inhibition Assay IC50=10 μM， IC90=36 μM 24961790
POS-1 Growth Inhibition Assay IC50=8 μM， IC90=36 μM 24961790
92.1 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
Omm1.3 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
C918 Growth Inhibition Assay 500-2000 nM 5 d inhibits the phosphorylation of AKT (Ser473) up to 1 μM 24563540
Mel290 Growth Inhibition Assay 500-2000 nM 5 d inhibits the phosphorylation of AKT (Ser473) up to 1 μM 24563540
OPM2 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
U266 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
MM1S Growth Inhibition Assay 0.5-2.5 μM 48 h inhibits cell growth in a dose-dependent manner 24405121
H929 Growth Inhibition Assay 0.5-2.5 μM 48 h inhibits cell growth in a dose-dependent manner 24405121
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
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
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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 441.47 화학식

C19H22F3N5O2S

 보관 (수령일로부터)
CAS 번호 1217486-61-7 SDF 다운로드 원액 보관

동의어 N/A Smiles CC1=C(SC(=N1)NC(=O)N2CCCC2C(=O)N)C3=CC(=NC=C3)C(C)(C)C(F)(F)F

용해도 (Solubility)

In vitro
배치:

DMSO : 88 mg/mL (199.33 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

Targets/IC50/Ki
PI3Kα
(Cell-free assay)
5 nM
시험관 내(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.

생체 내(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.

참조

적용 분야 (Applications)

방법 바이오마커 이미지 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)
S2814-WB5
27604488
Growth inhibition assay Cell viability
S2814-viability1
27602501
Immunofluorescence LC3
S2814-IF1
26637440

임상시험 정보 (Clinical Trial Information)

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호 모집 조건 스폰서/협력자 시작일 단계
NCT05948943 Recruiting
Lymphatic Malformations
Novartis Pharmaceuticals|Novartis
 November 24 2023 Phase 2|Phase 3
NCT05660083 Recruiting
HER2-negative Breast Cancer|Metastatic Breast Cancer|Metaplastic Breast Carcinoma|TNBC - Triple-Negative Breast Cancer
The Methodist Hospital Research Institute|Novartis Pharmaceuticals
 January 12 2023 Phase 2
NCT05508906 Recruiting
Metastatic Breast Cancer|Advanced Breast Cancer|HR-positive Breast Cancer|HER2-negative Breast Cancer
Olema Pharmaceuticals Inc.|Novartis
 August 31 2022 Phase 1
NCT05230810 Recruiting
HER2-positive Metastatic Breast Cancer
Criterium Inc.|Novartis|Seagen Inc.
 August 25 2022 Phase 1|Phase 2