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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PI3K-Alpelisib
Alpelisib

Chemical Structure : Alpelisib

CAS No.: 1217486-61-7

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Alpelisib (BYL-719, NVP-BYL719)

货号: PC-20590Not For Human Use, Lab Use Only.

Alpelisib (NVP-BYL719, BYL719) is ia potent, selective, and orally active PI3Kα inhibitor with IC50 of 5 nM, >50-fold selectivity over p110γ/p110δ/p110β.

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10 mg ￥980 In stock
25 mg ￥1580 In stock
50 mg ￥2580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Alpelisib (NVP-BYL719, BYL719) is ia potent, selective, and orally active PI3Kα inhibitor with IC50 of 5 nM, >50-fold selectivity over p110γ/p110δ/p110β.
Alpelisib (BYL719) potently inhibits PIK3CA somatic mutations (H1047R, E545K) with IC50 of 4 nM.
Alpelisib (BYL719) potently inhibits Akt phosphorylation in cells transformed with PI3Kα (IC50=74 nM) and shows significant reduced inhibitory activity in PI3Kβ or PI3Kδ isoforms transformed cells (>15-fold).
Alpelisib (BYL719) (0-50 uM) inhibits the cell growth of osteosarcoma cell lines MG63, HOS, POS-1 and MOS-J in a dose-dependent manner.
Alpelisib (BYL719) potently suppresses proliferation and PI3K signaling in human breast cancer cells harboring PIK3CA(H1047R) in combination with lapatinib.
Alpelisib (BYL719) inhibits growth factor-independent KRASG12D BM colony formation and sensitizes cells to a low dose of the MEK inhibitor MEK162.

物理化学性质&存储条件

分子量 441.47
分子式 C19H22F3N5O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(S)-N1-(4-methyl-5-(2-(1,1,1-trifluoro-2-methylpropan-2-yl)pyridin-4-yl)thiazol-2-yl)pyrrolidine-1,2-dicarboxamide

参考文献

1. Furet P, et al. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3741-8.

2. Gobin B, et al. Int J Cancer. 2015 Feb 15;136(4):784-96.

3. Fritsch C, et al. Mol Cancer Ther. 2014 May;13(5):1117-29.

4. Elkabets M, et al. Sci Transl Med. 2013 Jul 31;5(196):196ra99.

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