Alpelisib hydrochloride

SKU: orb1707687

描述

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	1584128-91-5
MW	477.93
纯度	97.64% (May vary between batches)
分子式	C₁₉H₂₃ClF₃N₅O₂S
SMILES	CC1=C(C=2C=C(C(C(F)(F)F)(C)C)N=CC2)SC(NC(=O)N3[C@H](C(N)=O)CCC3)=N1.Cl
靶点	PI3K

生物活性

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体内

Alpelisib has moderate terminal elimination half-life (t1/2=2.9±0.2 h) for rat (1 mg/kg, iv). Alpelisib (BYL-719) (12.5 mg/kg and 50 mg/kg for C57Bl/6J mice; 50 mg/kg for female Rj:NMRI-nude mice; oral administration; daily) significantly reduces tumor volumes and deposition of ectopic bone matrix.

体外

Alpelisib (BYL-719) potently inhibits the two most common PIK3CA somatic mutations (H1047R, E545K; IC50s~4 nM) and significantly alters the distribution of cell cycle phases. At 25 μM for 18 hours, it induces a G0/G1 phase cell cycle arrest in human and murine osteosarcoma cell lines. Additionally, Alpelisib (0-50 μM; 72 hours) inhibits the cell growth of osteosarcoma cell lines MG63, HOS, POS-1, and MOS-J in a dose-dependent manner. In cells transformed with PI3Kα, it potently inhibits Akt phosphorylation (IC50=74±15 nM) and shows significantly reduced inhibitory activity in PI3Kβ or PI3Kδ isoform-transformed cells (≥15-fold compared with PI3Kα).

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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BYL 719 Hydrochloride, BYL719 Hydrochloride, BYL-719 Hydrochloride, BYL-719 hydrochloride, Alpelisib hydrochloride, Alpelisib Hydrochloride

质量保证

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化合物标识

PubChem CID

139035009 ↗

关键属性

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暂无计算属性。

实验方案信息

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Alpelisib hydrochloride

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

质量保证

化合物标识

关键属性

实验方案信息

可选规格