PI3K-IN-1

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Chemical Structure| 1349796-36-6 同义名 : XL147 analog 2; SAR245409; SAR245409-Analog; XL765-Analog; Voxtalisib-Analog; Voxtalisib Analogue; XL-147 derivative 1
CAS号 : 1349796-36-6
货号 : A781923
分子式 : C31H29N5O6S
纯度 : 98+%
分子量 : 599.66
MDL号 : MFCD18252649
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(41.69 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • p110γ

    PI3Kγ, IC50:9 nM

  • p110β

    PI3Kβ, IC50:113 nM

  • p110α

    PI3Kα, IC50:39 nM

  • p110δ

    PI3Kδ, IC50:43 nM

  • mTOR

    mTOR, IC50:157 nM
描述 XL765 analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM, and also inhibits DNA-PK and mTOR.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.67mL

0.33mL

0.17mL

8.34mL

1.67mL

0.83mL

16.68mL

3.34mL

1.67mL
参考文献

[1]Prasad G, Sottero T, et al. Inhibition of PI3K/mTOR pathways in glioblastoma and implications for combination therapy with temozolomide. Neuro Oncol. 2011 Apr;13(4):384-92.

[2]Garcia-Echeverria C, Sellers WR. Drug discovery approaches targeting the PI3K/Akt pathway in cancer. Oncogene. 2008 Sep 18;27(41):5511-26.