1101810-02-9

1101810-02-9 structure

Name: AZD 3147
Chemical Name: AZD3147
CAS Number: 1101810-02-9
Molecular Formula: C₂₄H₃₁N₅O₄S₂
Molecular Weight: 517.664
Catalog: Signaling Pathways PI3K/Akt/mTOR mTOR
Create Date: 2018-01-27 17:44:38
Modify Date: 2024-01-05 16:55:24
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].

Name	AZD3147
Synonyms	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)-

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.