GDC-0349 - 10mM in DMSO , Serine/threonine-protein kinase mTOR inhibitor, CAS No.1207360-89-1, Serine/threonine-protein kinase mTOR inhibitor

CAS: 1207360-89-1 Cat. No.: G407793 Molecular Weight: 452.55

GRADE & PURITY 10mM in DMSO

Synonyms

RG-7603 | Urea, N-ethyl-N'-[4-[5,6,7,8-tetrahydro-4-[(3S)-3-methyl-4-morpholinyl]-7-(3-oxetanyl)pyrido[3,4-d]pyrimidin-2-yl]phenyl]-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

GDC-0349 GDC-0349 (RG-7603) is a potent and selective ATP-competitive inhibitor of mTOR with K i of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1.
In vitro

GDC-0349 has remarkable selectivity over 266 kinases, including all isoforms of PI3K. GDC-0349 inhibits 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.

In vivo

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 inhibits tumor growth in a dose-dependent manner. It is also efficacious in other xenograft models, including PC3 (PTEN ) and 786-O (VHL mutant).
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

RG-7603 | Urea, N-ethyl-N'-[4-[5, 6, 7, 8-tetrahydro-4-[(3S)-3-methyl-4-morpholinyl]-7-(3-oxetanyl)pyrido[3, 4-d]pyrimidin-2-yl]phenyl]-

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

GDC-0349 (RG-7603) is a potent and selective ATP-competitive inhibitor of mTOR with K_i of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Mechanism of action

Serine/threonine-protein kinase mTOR inhibitor

Names and Identifiers

• Isomeric SMILES: CCNC(=O)NC1=CC=C(C=C1)C2=NC3=C(CCN(C3)C4COC4)C(=N2)N5CCOC[C@@H]5C
• Molecular Weight: 452.55
• Reaxy-Rn: 52178663
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=52178663&ln=

Associated Targets(Human)

MTOR Tclin Serine/threonine-protein kinase mTOR (2 Activities)

Discover Target: MTOR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)