GDC-0349, mTOR Inhibitor


Catalog No. size PriceQuantity
M60110-2S 2mg solid $129
M60110-10S 10 mg solid $510

Description

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.

Product information

CAS Number: 1207360-89-1

Molecular Weight: 452.55

Formula: C24H32N6O3

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

Smiles: C[C@H]1COCCN1C1=NC(=NC2CN(CCC1=2)C1COC1)C1=CC=C(C=C1)NC(=O)NCC

InChiKey: RGJOJUGRHPQXGF-INIZCTEOSA-N

InChi: InChI=1S/C24H32N6O3/c1-3-25-24(31)26-18-6-4-17(5-7-18)22-27-21-12-29(19-14-33-15-19)9-8-20(21)23(28-22)30-10-11-32-13-16(30)2/h4-7,16,19H,3,8-15H2,1-2H3,(H2,25,26,31)/t16-/m0/s1

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 50 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

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.

References:

  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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