AZD 3147

Names

[ Name ]:
AZD 3147

[Synonym ]:
1-(4-{4-[1-(Cyclopropylsulfonyl)cyclopropyl]-6-[(3S)-3-methyl-4-morpholinyl]-2-pyrimidinyl}phenyl)-3-(2-hydroxyethyl)thiourea
Thiourea, N-[4-[4-[1-(cyclopropylsulfonyl)cyclopropyl]-6-[(3S)-3-methyl-4-morpholinyl]-2-pyrimidinyl]phenyl]-N'-(2-hydroxyethyl)-

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> PI3K/Akt/mTOR >> mTOR

Research Areas >> Cancer

[Target]

mTORC1

mTORC2

[In Vitro]

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].

[In Vivo]

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

[References]

[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.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
696.7±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₄H₃₁N₅O₄S₂

[ Molecular Weight ]:
517.664

[ Flash Point ]:
375.2±34.3 °C

[ Exact Mass ]:
517.181763

[ LogP ]:
-0.58

[ Vapour Pressure ]:
0.0±2.3 mmHg at 25°C

[ Index of Refraction ]:
1.689

Related Compounds

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