Immunoway/Alpelisib(BYL-719)/10mg 50mg 100mg/MC0318
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¥3600.00
美元价：
1800.00
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3392242852
电话号码：
4000-520-616
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商品介绍
Alpelisib(BYL-719)
- Catalog No.：MC0318
- Data Sheet
- MSDS
- Support
- Description
- References ( 0 )
- Protocol
- CasNo：
- 1217486-61-7
- MolecularFormula：
- C19H22F3N5O2S
- Purity：
- >98%
- Target：
- PI3K
- IC50：
- IC50: 5 nM (p110α), 250 (p110γ), 290 (p110δ), 1200 (p110β)[1]
- In Vitro：
- BYL-719 (NVP-BYL719) potently inhibits the 2 most common PIK3CA somatic mutations (H1047R, E545K; IC50∼4 nM). BYL-719 potently inhibits Akt phosphorylation in cells transformed with PI3Kα (IC50=74±15 nM) and shows significant reduced inhibitory activity in PI3Kβ or PI3Kδ isoforms transformed cells (≥15-fold compared with PI3Kα)[2]. BYL-719 (BYL719) decreases cell proliferation by blocking cell cycle in G0/G1 phase with no outstanding effects on apoptosis cell death in HOS and MOS-J tumor cells. BYL-719 inhibits cell migration and can thus be considered as a cytostatic drug for osteosarcoma. In murine preclinical models of osteosarcoma, BYL-719 significantly decreases tumor progression and tumor ectopic bone formation as shown by a decrease of Ki67+ cells and tumor vascularization. BYL-719 rapidly inhibits the levels of P-AKT and P-mTOR in all cell lines assessed, confirming the functional activity of BYL-719 on osteosarcoma cells. After 72 hr of treatment, BYL-719 significantly inhibit
- In Vivo：
- BYL-719 displays excellent oral bioavailability in rats, mice and dogs and does not show any significant inhibition of the CYP450 enzymes[1]. BYL-719 (BYL719) inhibits tumor growth in pre-clinical murine models of osteosarcoma. C57Bl/6J with MOS-J tumors (n=6 per group) are randomized as controls (vehicle) or BYL-719 (12.5 mg/kg or 50 mg/kg per day)[3].
- Fields：
- BYL719 is a potent and selective PI3Kα inhibitor with IC50 of 5 nM, ;liitle or no effect on PI3Kβ/γ/δ.
- Specificity：
- Target:PI3K. Fields: BYL719 is a potent and selective PI3Kα inhibitor with IC50 of 5 nM, ;liitle or no effect on PI3Kβ/γ/δ.
- Source：
- Rabbit
- Dilution：
- IC50: 5 nM (p110α), 250 (p110γ), 290 (p110δ), 1200 (p110β)[1]
- Concentration：
- >98%
- Storage Stability：
- 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
- Other Name：
- BYL 719; BYL719
- MolecularWeight(Da)：
- 441.47
- References：
- [1]. Furet P, et al. Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3741-8.[2].
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品牌分类
\Elisa试剂盒\
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