GDC-0349

MTOR inhibitor CAS# 1207360-89-1

GDC-0349

Catalog No. BCC1094----Order now to get a substantial discount!

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Quality Control of GDC-0349

Number of papers citing our products

Chemical structure

GDC-0349

3D structure

Chemical Properties of GDC-0349

Cas No. 1207360-89-1 SDF Download SDF
PubChem ID 59239165 Appearance Powder
Formula C24H32N6O3 M.Wt 452.55
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 100 mg/mL (220.97 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 1-ethyl-3-[4-[4-[(3S)-3-methylmorpholin-4-yl]-7-(oxetan-3-yl)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-2-yl]phenyl]urea
SMILES CCNC(=O)NC1=CC=C(C=C1)C2=NC3=C(CCN(C3)C4COC4)C(=N2)N5CCOCC5C
Standard InChIKey RGJOJUGRHPQXGF-INIZCTEOSA-N
Standard 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
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of GDC-0349

DescriptionGDC-0349 is a potent and selective ATP-competitive inhibitor of mTOR with Ki value of 3.8 nM.
TargetsmTOR    
IC503.8 nM (Ki)     

GDC-0349 Dilution Calculator

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GDC-0349 Molarity Calculator

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Preparing Stock Solutions of GDC-0349

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.2097 mL 11.0485 mL 22.097 mL 44.194 mL 55.2425 mL
5 mM 0.4419 mL 2.2097 mL 4.4194 mL 8.8388 mL 11.0485 mL
10 mM 0.221 mL 1.1049 mL 2.2097 mL 4.4194 mL 5.5243 mL
50 mM 0.0442 mL 0.221 mL 0.4419 mL 0.8839 mL 1.1049 mL
100 mM 0.0221 mL 0.1105 mL 0.221 mL 0.4419 mL 0.5524 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on GDC-0349

GDC-0349 is a potent, selective, ATP-competitive inhibitor of (Mammalian target of rapamycin) mTOR with Ki value of 3.8nM [1].

GDC-0349 is a remarkably selective mTOR inhibitor, with less than 25% inhibition of 266 kinases, including all isoforms of PI3K. GDC-0349 inhibited mTOR downstream markers , involving phospho-Akt(s473) and phospho-4EBP1 in an in vivo PK/PD study in mouse, consistent with an inhibition of mTORC1/mTORC2 complexes [1].

GDC-0349 inhibited tumor growth in a dose-dependent manner when dosed orally once daily in athymic mice in a MCF7-neo/Her2 tumor xenograft model (PI3K mutation). GDC-0349 was also efficacious in other xenograft models, including PC3 (PTEN null) and 786-0 (VHL mutant). However, GDC-0349 showed only modest tumor growth delay in the A549 mouse xenograft model (KRas mutant, LKB1 deficient) [1].

References:
[1] Pei, Z.; Blackwood, E.; Liu, L.; Malek, S.; Belvin, M.; Koehler, M. F. T.; Ortwine, D. F.; Chen, H.; Cohen, F.; Kenny, J. R.; Bergeron, P.; Lau,K.; Ly, C.; Zhao, X.; Estrada, A. A.; Truong, T.; Epler, J. A.; Nonomiya, J.; Trinh, L.; Sideris, S.; Lesnick, J.; Bao, L.; Vijapurkar, U.; Mukadam,S.; Tay, S.; Deshmukh, G.; Chen, Y.-H.; Ding, X.; Friedman, L.; Lyssikatos, J. P.Discovery and biological profiling of potent and selective mTOR inhibitor GDC-0349 ACS Med. Chem. Lett. 2013, 4, 103– 107

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References on GDC-0349

Autophagy induction contributes to GDC-0349 resistance in head and neck squamous cell carcinoma (HNSCC) cells.[Pubmed:27291151]

Biochem Biophys Res Commun. 2016 Aug 19;477(2):174-80.

Dysregulation of mammalian target of rapamycin (mTOR) signaling contributes to head and neck squamous cell carcinoma (HNSCC) tumorigenesis and progression. In the current study, we tested the anti-HNSCC cell activity by GDC-0349, a selective ATP-competitive inhibitor of mTOR. We showed that GDC-0349 inhibited proliferation of established and primary human HNSCC cells bearing high-level of p-AKT/p-S6K. Further, it induced caspase-dependent apoptosis in the HNSCC cells. GDC-0349 blocked mTORC1 and mTORC2 activation, yet it simultaneously induced autophagy activation in HNSCC cells. The latter was evidenced by induction of LC3B-II, Beclin-1 and Autophagy-related (ATG)-7, as well as downregulation of p62. Autophagy inhibitors (3-methyladenine and bafilomycin A1) or ATG-7 siRNA dramatically potentiated GDC-0349's cytotoxicity against HNSCC cells. Intriguingly, we showed that ceramide (C14), a pro-apoptotic sphingolipid, also induced ATG-7 degradation, and sensitized HNSCC cells to GDC-0349. Collectively, the preclinical study provided evidences to support GDC-0349 as a promising anti-HNSCC agent. GDC-0349 sensitization may be achieved via autophagy inhibition.

Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.[Pubmed:24900569]

ACS Med Chem Lett. 2012 Nov 29;4(1):103-7.

Aberrant activation of the PI3K-Akt-mTOR signaling pathway has been observed in human tumors and tumor cell lines, indicating that these protein kinases may be attractive therapeutic targets for treating cancer. Optimization of advanced lead 1 culminated in the discovery of clinical development candidate 8h, GDC-0349, a potent and selective ATP-competitive inhibitor of mTOR. GDC-0349 demonstrates pathway modulation and dose-dependent efficacy in mouse xenograft cancer models.

Description

GDC-0349 is a potent and selective ATP-competitive mTOR inhibitor with a Ki of 3.8 nM. GDC-0349 inhibits of both mTORC1 and mTORC2 complexes.

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