For research use only. Not for therapeutic Use.
AZD3147 is a potent, orally active, selective dual inhibitor of mTORC1 and mTORC2 with an IC50 value of 1.5 nM. AZD3147 also has a selective effect on PI3K[1].
AZD3147 (0-50 nM, 1 h) can alleviate fibroblast growth factor (FGF)-mediated cilia extension at concentrations above 1.5 nM in NIH3T3 cells[2].
AZD3147 inhibits cell viability of neuroblastoma cell lines Kelly and IMR-32 with the IC50 values of 0.88 nM and 662.4 nM, respectively[3].
The pharmacokinetic parameters of AZD3147[1].
Parameter
Mouse
Dog
CL (mL/min/kg)
78
16
Vss (L/kg)
2.3
2.2
t1/2(h)
0.9
1.9
F%
61
73
| Catalog Number | I003026 |
| CAS Number | 1101810-02-9 |
| Synonyms | 1-[4-[4-(1-cyclopropylsulfonylcyclopropyl)-6-[(3S)-3-methylmorpholin-4-yl]pyrimidin-2-yl]phenyl]-3-(2-hydroxyethyl)thiourea |
| Molecular Formula | C24H31N5O4S2 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H31N5O4S2/c1-16-15-33-13-11-29(16)21-14-20(24(8-9-24)35(31,32)19-6-7-19)27-22(28-21)17-2-4-18(5-3-17)26-23(34)25-10-12-30/h2-5,14,16,19,30H,6-13,15H2,1H3,(H2,25,26,34)/t16-/m0/s1 |
| InChIKey | JWGVUDPAMQEIJU-INIZCTEOSA-N |
| SMILES | CC1COCCN1C2=NC(=NC(=C2)C3(CC3)S(=O)(=O)C4CC4)C5=CC=C(C=C5)NC(=S)NCCO |
| Reference | [1]. Kurt G Pike, et al. Discovery of AZD3147: a potent, selective dual inhibitor of mTORC1 and mTORC2. J Med Chem. 2015 Mar 12;58(5):2326-49. [2]. Michaela Kunova Bosakova, et al. Regulation of ciliary function by fibroblast growth factor signaling identifies FGFR3-related disorders achondroplasia and thanatophoric dysplasia as ciliopathies. Hum Mol Genet. 2018 Mar 15;27(6):1093-1105. [3]. Rebecca Waetzig, et al. Comparing mTOR inhibitor Rapamycin with Torin-2 within the RIST molecular-targeted regimen in neuroblastoma cells. Int J Med Sci. 2021 Jan 1;18(1):137-149. |
