| Identification | Back Directory | [Name]
AZD-8055 | [CAS]
1009298-09-2 | [Synonyms]
CS-1935
CCG 168
AZD-8055
AZD8055, >=98%
AZD8055,AZD-8055
AZD-8055 USP/EP/BP
AZD-8055; AZD8055; AZD 8055.
[5-[2,4-Bis((3S)-3-MethylMorpholin-4-yl)pyrido[
(5-(2,4-Bis((S)-3-methylmorpholino)pyrido-[2,3-d]pyrimidin-7-yl)-2-methoxyphenyl)methanol
(5-{2,4-dichloropyrido[2,3-d]pyriMidin-7-yl}-2-Methoxyphenyl)Methyl 2,2-diMethylpropanoate
5-[2,4-Bis[(3S)-3-Methyl-4-Morpholinyl]pyrido[2,3-d]pyriMidin-7-yl]-2-MethoxybenzeneMethanol
{5-[2,4-Bis-(3-methyl-morpholin-4-yl)-pyrido[2,3-d]pyrimidin-7-yl]-2-methoxy-phenyl}-methanol
[5-[2,4-Bis((3S)-3-methylmorpholin-4-yl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxyphenyl]methanol
(5-{2,4-Bis[(3S)-3-methyl-4-morpholinyl]pyrido[2,3-d]pyrimidin-7-yl}-2-methoxyphenyl)methanol
Benzenemethanol, 5-[2,4-bis[(3S)-3-methyl-4-morpholinyl]pyrido[2,3-d]pyrimidin-7-yl]-2-methoxy-
Propanoic acid, 2,2-dimethyl-, [5-(2,4-dichloropyrido[2,3-d]pyrimidin-7-yl)-2-methoxyphenyl]methyl ester
[5-[2,4-Bis((3S)-3-methylmorpholin-4-yl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxyphenyl]methanol AZD 8055
AZD 8055 [5-[2,4-Bis((3S)-3-methylmorpholin-4-yl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxyphenyl]methanol | [Molecular Formula]
C25H31N5O4 | [MDL Number]
MFCD16660191 | [MOL File]
1009298-09-2.mol | [Molecular Weight]
465.54 |
| Chemical Properties | Back Directory | [Melting point ]
204 - 207°C | [Boiling point ]
694.3±65.0 °C(Predicted) | [density ]
1.248 | [storage temp. ]
-20°C | [solubility ]
Soluble in DMSO (up to 30 mg/ml) | [form ]
Yellow powder. | [pka]
14.20±0.10(Predicted) | [color ]
Yellow | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months. |
| Hazard Information | Back Directory | [Description]
AZD8055 (1009298-09-2) is a potent and highly selective inhibitor of mammalian target of rapamycin kinase (mTOR) kinase (IC50 = 0.8 nM).1,2 ?mTOR acts as a nutrient/energy/redox sensor and a controller of protein synthesis – as such it is a very important target for cancer research.? It has been investigated as a potential chemotherapeutic for various cancers.3-7 | [Uses]
A novel ATP-competitive inhibitor of mTOR with an IC50 of 0.8 nM. | [Uses]
A potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM. It inhibits the phosphorylation of mTORC1 substrates p70S6K and 4E-BP1 as well as phosphoryla
tion of the mTORC2 substrate AKT and downstream proteins. The rapamycin-resistant T37/46 phosphorylation sites on 4E-BP1 were fully inhibited by AZD8055, resulting in significant inhibition of cap-dep
endent translation. In vitro, AZD8055 potently inhibits proliferation and induces autophagy in H838 and A549 cells. In vivo, AZD8055 induces a dose-dependent pharmacodynamic effect on phosphorylated S
6 and phosphorylated AKT at plasma concentrations leading to tumor growth inhibition. | [Definition]
ChEBI: AZD-8055 is a pyridopyrimidine that is pyrido[2,3-d]pyrimidine which is substituted at positions 2 and 4 by (3S)-3-methylmorpholin-4-yl groups and at position 5 by a 3-(hydroxymethyl)-4-methoxyphenyl group. It is an mTOR complex 1/2 (mTORC1/2) dual inhibitor [mTOR = mammalian target of rapamycin]. It has a role as a mTOR inhibitor, an apoptosis inducer and an antineoplastic agent. It is a member of benzyl alcohols, a tertiary amino compound, a pyridopyrimidine and a member of morpholines. | [target]
mTOR (full length) | [storage]
Store at -20°C | [References]
1) Chresta et al. (2010), AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mammalian target of rapamycin kinase inhibitor with in vitro and in vivo antitumor activity; Cancer Res. 70 288
2) Pike et al. (2013), Optimization of potent an selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014; Bioorg. Med. Chem. Lett. 23 1212
3) Holt et al. (2012), Enhanced apoptosis and tumor growth suppression elicited by combination of MEK (selumetinib) and mTOR kinase inhibitors (AZD8055); Cancer Res. 72 1804
4) Willems et al. (2012), The dual mTORC1 and mTORC2 inhibitor AZD8055 has anti-tumor activity in acute myeloid leukemia; Leukemia 26 1195
5) Li et al. (2013),The mTOR inhibitor AZD8055 inhibits proliferation and glycolysis in cervical cancer cells; Oncol. Lett. 5 717
6) Li et al. (2013), The dual mTORC1 and mTORC2 inhibitor AZD8055 inhibits head and neck squamous cell carcinoma cell growth in vivo and in vitro; Biochem. Biophys. Res. Commun. 440 701
7) Hu et al. (2014), AZD8055 induces cell death associated with autophagy and activation of AMPK in hepatocellular carcinoma; Oncol. Rep. 31 649 |
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