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GDC-0349, mTOR Inhibitor

GDC-0349, mTOR Inhibitor

$129.00
A potent and selective ATP-competitive inhibitor of mTOR in clinical trials.
Catalog No. Unit Price Qty
M60110-2s 2mg solid $129.00
M60110-50s 50mg solid $950.00

Details

Product Information
Molecular Weight: 452.55
Formula: C24H32N6O3
Purity: ≥98%
CAS#: 1207360-89-1
Solubility: DMSO up to 50 mM
Chemical Name: (S)-1-ethyl-3-(4-(4-(3-methylmorpholino)-7-(oxetan-3-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)phenyl)urea
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

GDC-0349 is a potent and selective ATP-competitive inhibitor of mTOR with IC50 ~3.8 nM. It has remarkable selectivity over 266 kinases, including all isoforms of PI3K (less than 25% inhibition when tested at 1 μM against Invitrogen kinase panel). GDC-0349 demonstrates pathway modulation and dose-dependent efficacy in mouse xenograft cancer models.  When dosed orally once daily in athymic mice in a MCF7-neo/Her2 tumor xenograft model (PI3K mutation), GDC-0349 inhibited tumor growth in a dose-dependent manner. It was also efficacious in other xenograft models, including PC3 (PTEN null) and 786-0 (VHL mutant). GDC-0349 inhibited downstream markers of mTOR, including phospho-4EBP1 and phospho-Akt(S473) in an in vivo PK/PD study in mouse, consistent with an inhibition of both mTORC1 and mTORC2 complexes. Currently GDC-0349 is in Phase I clinical trials to evaluate the safety and tolerability in patients with locally advanced or metastatic solid tumors or Non-Hodgkin's lymphoma. 

 

How to Use:

  • In vitro: GDC-0349 was used at 1 µM in vitro and in cellular assays. 
  • In vivo: GDC-0349 was orally dosed to mice at 30-80 mg/kg once per day.

 

Reference:

  •  1. Zhonghua Pei, et al. Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349 (2013) ACS Med. Chem. Lett., 4 (1), pp 103–107

 




Products are for research use only. Not for human use.

Description

Details

Product Information
Molecular Weight: 452.55
Formula: C24H32N6O3
Purity: ≥98%
CAS#: 1207360-89-1
Solubility: DMSO up to 50 mM
Chemical Name: (S)-1-ethyl-3-(4-(4-(3-methylmorpholino)-7-(oxetan-3-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)phenyl)urea
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

GDC-0349 is a potent and selective ATP-competitive inhibitor of mTOR with IC50 ~3.8 nM. It has remarkable selectivity over 266 kinases, including all isoforms of PI3K (less than 25% inhibition when tested at 1 μM against Invitrogen kinase panel). GDC-0349 demonstrates pathway modulation and dose-dependent efficacy in mouse xenograft cancer models.  When dosed orally once daily in athymic mice in a MCF7-neo/Her2 tumor xenograft model (PI3K mutation), GDC-0349 inhibited tumor growth in a dose-dependent manner. It was also efficacious in other xenograft models, including PC3 (PTEN null) and 786-0 (VHL mutant). GDC-0349 inhibited downstream markers of mTOR, including phospho-4EBP1 and phospho-Akt(S473) in an in vivo PK/PD study in mouse, consistent with an inhibition of both mTORC1 and mTORC2 complexes. Currently GDC-0349 is in Phase I clinical trials to evaluate the safety and tolerability in patients with locally advanced or metastatic solid tumors or Non-Hodgkin's lymphoma. 

 

How to Use:

  • In vitro: GDC-0349 was used at 1 µM in vitro and in cellular assays. 
  • In vivo: GDC-0349 was orally dosed to mice at 30-80 mg/kg once per day.

 

Reference:

  •  1. Zhonghua Pei, et al. Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349 (2013) ACS Med. Chem. Lett., 4 (1), pp 103–107

 




Products are for research use only. Not for human use.

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