PI3K/mTOR Inhibitor-13

Names

[ CAS No. ]:
1621718-37-3

[ Name ]:
PI3K/mTOR Inhibitor-13

Biological Activity

[Description]:

PI3K/mTOR Inhibitor-13 is an orally active dual inhibitor of phosphoinositol 3-kinase (PI3K) and mTOR kinase. PI3K/mTOR Inhibitor-13 has potential applications in sexual diseases, solid tumor and idiopathic pulmonary fibrosis (IPF)[1][2].

[Related Catalog]:

Signaling Pathways >> PI3K/Akt/mTOR >> mTOR
Research Areas >> Cancer
Signaling Pathways >> PI3K/Akt/mTOR >> PI3K

[In Vitro]

PI3K/mTOR Inhibitor-13 (Compound A) (0-2 µM；48 h) 以剂量依赖性方式抑制 HFL1 细胞的增值[1]。 Cell Proliferation Assay[1] Cell Line: HFL1 cells. Concentration: 0, 0.03125, 0.0125, 0.025, 0.05, 0.0625, 0.1, 0.125, 0.2, 0.25, 0.4, 0.5, 1 and 2 µM. Incubation Time: 48 h. Result: Showed inhibitory for HFL1 cells. Western Blot Analysis[1] Cell Line: HFL1 cells. Concentration: 200 nM. Incubation Time: 48 h. Result: Increased the expression of α-SMA/Tubulin.

[In Vivo]

PI3K/mTOR Inhibitor-13 的药代动力学 (PK) 参数[2] Species Administration manner Dose (mg/kg) T1/2 (h) AUClast (ng•h/mL) Cl/F (L/h/kg) Vss (L/kg) F (%) Rat Intravenous injection 2 2.77 7069 0.29 0.85 94.75 Mice Intravenous injection 1 5.45 57059 0.02 0.13 79.3 Dog Intravenous injection 1 0.67 3672 0.27 0.23 108.5 Monkey Intravenous injection 1 9.70 5978 0.16 0.92 59.8

[References]

[1]. Cao S, et al. Pharmaceutical combination or pharmaceutical composition for treatment of fibrotic diseases. World Intellectual Property Organization. WO2020078445.

[2]. Xi N, et al. Aromatic heterocyclic compounds, pharmaceutical composition containing compounds and application of pharmaceutical composition.China.CN103965199.

Chemical & Physical Properties

[ Molecular Formula ]:
C20H13F2N5O3S

[ Molecular Weight ]:
441.41

Related Compounds