CAS |
1217486-61-7 |
Chinese Name |
阿吡利塞 |
English Name |
Alpelisib |
Synonym |
BYL-719 |
Unit |
Bottle |
Purity |
≥98% |
Molecular Formula |
C19H22F3N5O2S |
Molecular Weight |
441.47 |
Appearance |
White to yellow solid |
Storage |
Powder : 2-8℃, 2 years; In solvent(mother liquid): -20℃, 1 month; -80℃, 6 months |
Solubility |
Soluble in DMSO |
MDL |
MFCD22417085 |
InChIKey |
STUWGJZDJHPWGZ-LBPRGKRZSA-N |
InChI |
InChI=1S/C19H22F3N5O2S/c1-10-14(11-6-7-24-13(9-11)18(2,3)19(20,21)22)30-16(25-10)26-17(29)27-8-4-5-12(27)15(23)28/h6-7,9,12H,4-5,8H2,1-3H3,(H2,23,28)(H,25,26,29)/t12-/m0/s1 |
PubChem CID |
56649450 |
Delivery Time |
1-2 days |
SMILES |
CC(N=C(S1)NC(N2CCC[C@H]2C(N)=O)=O)=C1C3=CC(C(C)(C(F)(F)F)C)=NC=C3 |
Description |
Alpelisib is a potent and selective PI3Kα inhibitor. |
Target Point |
PI3K |
Passage |
PI3K/Akt/mTOR |
IC50 |
p110α:5 nM ; p110γ:250 nM ; p110δ:290 nM ; p110β:1200 nM [1-5] |
Data Literature Source |
[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]. Fritsch C, et al. Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials. Mol Cancer Ther. 2014 May;13(5):1117-29.
[3]. Gobin B, et al. BYL719, a new α-specific PI3K inhibitor: single administration and in combination with conventional chemotherapy for the treatment of osteosarcoma. Int J Cancer. 2015 Feb 15;136(4):784-96.
[4]. Venot Q, et al. Targeted therapy in patients with PIK3CA-related overgrowth syndrome. Nature. 2018 Jun;558(7711):540-546.
[5]. Ding J, et al. Inhibition of BTF3 sensitizes luminal breast cancer cells to PI3Kα inhibition through the transcriptional regulation of ERα. Cancer Lett. 2018 Oct 10;440-441:54-63. |
Specification |
1mg 5mg 10mg |