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GDC-0349

Catalog No. T6510 CAS 1207360-89-1

Synonyms: RG-7603

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

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GDC-0349, CAS 1207360-89-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 41.00
2 mg	In stock	$ 56.00
5 mg	In stock	$ 102.00
10 mg	In stock	$ 183.00
25 mg	In stock	$ 378.00
50 mg	In stock	$ 567.00
100 mg	In stock	$ 813.00
500 mg	In stock	$ 1,680.00
1 mL * 10 mM (in DMSO)	In stock	$ 108.00

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Purity: 98.98%

Purity: 96.00%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GDC-0349 (RG-7603) is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1.
Targets&IC50	mTOR:3.8 nM(Ki)
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. [1]
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 null) and 786-O (VHL mutant). [1]

Synonyms	RG-7603
Molecular Weight	452.55
Formula	C24H32N6O3
CAS No.	1207360-89-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 6 mg/mL (13.25 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 84 mg/mL (185.6 mM)

References and Literature

1. Zhonghua Pei, et al. J Med Chem, 2013, 56(7), 3090-3101. 2. Wang Z, Feng J, Yu J, et al. FKBP12 mediates necroptosis by initiating RIPK1–RIPK3–MLKL signal transduction in response to TNF receptor 1 ligation[J]. Journal of cell science. 2019 May 20;132(10). pii: jcs227777.

Citations

1. Wang Z, Feng J, Yu J, et al. FKBP12 mediates necroptosis by initiating RIPK1-RIPK3-MLKL signal transduction in response to TNF receptor 1 ligation. Journal of Cell Science. 2019, 132(10): jcs227777

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Highly Selective Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Kinase Inhibitor Library Anti-Cancer Active Compound Library Inhibitor Library Anti-Aging Compound Library Antioxidant Compound Library Covalent Inhibitor Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

GDC-0349 1207360-89-1 Autophagy PI3K/Akt/mTOR signaling PI3K mTOR Mammalian target of Rapamycin RG-7603 inhibit RG 7603 GDC0349 RG7603 GDC 0349 Inhibitor inhibitor

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