Alpelisib

SKU: orb1307105

描述

Alpelisib (BYL-719) is an orally bioavailable, potent, and selective PI3Kα inhibitor (IC50=5 nM) with significantly lower activity against other PI3K isoforms. It demonstrates antitumor efficacy in both in vitro and in vivo models, specifically targeting cancers harboring PIK3CA mutations.

研究领域

Pharmacology & Drug Discovery, Signal Transduction

图片与验证

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关键属性

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CAS 号	1217486-61-7
MW	441.47
纯度	99.86% (May vary between batches)
分子式	C₁₉H₂₂F₃N₅O₂S
SMILES	Cc1nc(NC(=O)N2CCC[C@H]2C(N)=O)sc1-c1ccnc(c1)C(C)(C)C(F)(F)F
靶点	PI3K
溶解性	Ethanol:2 mg/mL (4.53 mM);DMSO:240 mg/mL (543.64 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:8.2 mg/mL (18.57 mM)

生物活性

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靶点 IC50	p110δ:290 nM\|p110α:5 nM (cell free)\|p110α-E545K:4 nM\|p110γ:250 nM (cell free)\|p110α-H1047R:4 nM\|p110β:1200 nM
体内	METHODS: To assay anti-tumor activity in vivo, Alpelisib (12.5-50 mg/kg, methylcellulose 0.5%) was administered orally to Rj:NMRI-nude mice bearing human osteosarcoma HOS-MNNG once daily for twenty-two days. RESULTS: Alpelisib significantly reduced tumor volume in a dose-dependent manner. METHODS: To investigate the modulatory effects on collagen, Alpelisib (12.5-50 mg/kg) was administered orally to nude mice bearing subcutaneous xenografts of Rat1-myr-p110α tumors once daily for eight days. RESULTS: Treatment with 12.5, 25, and 50 mg/kg of Alpelisib was well tolerated and produced dose-dependent and statistically significant antitumor effects with a T/C of 14.1% and regressions of 9.6% and 65.2%, respectively.
体外	METHODS: Osteosarcoma cell lines MG-63, HOS, MOS-J and POS-1 were treated with Alpelisib (0-50 µM) for 72 h and cell viability was measured using XTT assay. RESULTS: Alpelisib significantly inhibited cell growth of all osteosarcoma cell lines in a dose-dependent manner with IC50 ranging from 6-15 µM and IC90 ranging from 24-42 µM. METHODS: PIK3CA wild-type cells (SNU638 and SNU668) and three PIK3CA mutant cells (SNU601, AGS, and MKN1) were treated with Alpelisib (5 µM) for 24 h, and cell cycle profiles were examined using Flow cytometry. RESULTS: Alpelisib treatment induced G0/G1 cell cycle arrest regardless of PIK3CA mutation status. In PIK3CA mutant cells (AGS and MKN1), there was a significant increase in the sub-G1 fraction, suggesting that Alpelisib increased apoptosis in these cell lines.
细胞研究	To evaluate the isoform-specific potency of NVP-BYL719 in a cell-based system, an N-terminally myristoylated form of each PI3K class IA isoform was expressed in Rat1 fibroblasts. The retroviral expression plasmid pBabePuro containing human p110α, p110β, and p110δ with an N-terminal myristoylation (myr) signal followed by an HA-tag were generated. Successfully infected Rat1 cells were selected in medium containing 4 μg/mL of puromycin, expanded and characterized for expression of the p110 isoforms. Transgenic expression of the myristoylated protein was confirmed by increased levels of phosphorylated Akt .
动物研究	All in life experimentation and efficacy studies were conducted as described previously. Tumor xenografts were grown subcutaneously or orthotopically in nude mice or nude Rowett rats (Hsd: RH-Fox1rnu) by injection of 3 × 10^6 to 1 × 10^7 cells or implantation of tumor fragments of approximately 50 mg. Tumor-bearing animals mice were treated with either vehicle control, NVP-BYL719, or NVP-BKM120 (p.o., every day) at the doses indicated .

储存与操作

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储存	-20°C
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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Inhibitor, mutant, inhibit, metastasis, breast, antineoplastic, cancer, BYL 719, BYL719, BYL-719, Alpelisib, AKT, Phosphoinositide 3-kinase, PI3K, phosphorylation, PIK3CA, PI3Kα, p110α

相似产品

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STX-478 [orb1910725]
纯度：
0.98
CAS 号：
2883540-92-7
MW:
401.297
分子式：
C₁₆H₁₂F₅N₅O₂
可选规格： 5 mg
Alpelisib carboxylic acid [orb3217472]
CAS 号：
2715981-74-9
MW:
442.46
分子式：
C₁₉H₂₁F₃N₄O₃S
可选规格： 50 mg, 10 mg
Alpelisib [orb2985790]
纯度：
>98%
CAS 号：
1217486-61-7
MW:
441.47
分子式：
C₁₉H₂₂F₃N₅O₂S
可选规格： 5 mg, 25 mg
Alpelisib hydrochloride [orb1707687]
纯度：
97.64% (May vary between batches)
CAS 号：
1584128-91-5
MW:
477.93
分子式：
C₁₉H₂₃ClF₃N₅O₂S
可选规格： 50 mg, 100 mg, 25 mg, 5 mg, 2 mg, 10 mg
BYL-719 [orb1226776]
纯度：
>98% (HPLC)
CAS 号：
1217486-61-7
MW:
441.47
分子式：
C₁₉H₂₂F₃N₅O₂S
可选规格： 10 mg, 25 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g, 5 mg

质量保证

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our 条款与条件和选购指南.

化合物标识

PubChem CID

56649450 ↗

关键属性

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暂无计算属性。

实验方案信息

查看更多实验方案

纯度：	0.98
CAS 号：	2883540-92-7
MW:	401.297
分子式：	C₁₆H₁₂F₅N₅O₂

CAS 号：	2715981-74-9
MW:	442.46
分子式：	C₁₉H₂₁F₃N₄O₃S

纯度：	>98%
CAS 号：	1217486-61-7
MW:	441.47
分子式：	C₁₉H₂₂F₃N₅O₂S

纯度：	97.64% (May vary between batches)
CAS 号：	1584128-91-5
MW:	477.93
分子式：	C₁₉H₂₃ClF₃N₅O₂S

纯度：	>98% (HPLC)
CAS 号：	1217486-61-7
MW:	441.47
分子式：	C₁₉H₂₂F₃N₅O₂S

Alpelisib

描述

研究领域

图片与验证

关键属性

生物活性

储存与操作

别名

相似产品

STX-478 [orb1910725]

Alpelisib carboxylic acid [orb3217472]

Alpelisib [orb2985790]

Alpelisib hydrochloride [orb1707687]

BYL-719 [orb1226776]

质量保证

化合物标识

关键属性

实验方案信息

可选规格