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

Chemical Structure : Voxtalisib

CAS No.: 934493-76-2

Voxtalisib (XL765;SAR245409;SAR-245409;XL 765;XL-765)

货号: PC-44791Not For Human Use, Lab Use Only.

Voxtalisib (XL765, SAR245409) is a potent, highly selective ATP-competitive inhibitor of class I PI3Ks with IC50s of 39/110/43/9 nM for p110α/p110β/p110δ/p120γ.

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10 mg ¥1280 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

Voxtalisib (XL765, SAR245409) is a potent, highly selective ATP-competitive inhibitor of class I PI3Ks with IC50s of 39/110/43/9 nM for p110α/p110β/p110δ/p120γ.
Voxtalisib (XL765, SAR245409) also inhibits mTORC1/mTORC2/DNA-PK (IC50=160/910/150 nM) and shows weak inhibitory activity toward VPS34 (IC50=9.1 uM).
Voxtalisib (XL765, SAR245409) inhibits phosphorylation of AKT, p70S6K, and S6 phosphorylation in multiple tumor cell lines.
Voxtalisib (XL765, SAR245409) is orally bioactive in mouse xenograft models.

物理化学性质&存储条件

分子量 270.2899
分子式 C13H14N6O
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

DMSO: 16 mg/mL

Chemical Name/SMILES

Pyrido[2,3-d]pyrimidin-7(8H)-one, 2-amino-8-ethyl-4-methyl-6-(1H-pyrazol-3-yl)-

参考文献

1. Yu P, et al. Mol Cancer Ther. 2014 May;13(5):1078-91.

2. Papadopoulos KP, et al. Clin Cancer Res. 2014 May 1;20(9):2445-56.

3. Thijssen R, et al. Leukemia. 2016 Feb;30(2):337-45.

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