AZD8055An mTOR kinase inhibitor

AZD8055 (CAS 1009298-09-2)

AZD8055 | CAS 1009298-09-2 is rated 5.0 out of 5 by 2.
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Synonym: (5-(2,4-bis((3S)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol
Application: An mTOR kinase inhibitor
CAS Number: 1009298-09-2
Purity: ≥98%
Molecular Weight: 465.54
Molecular Formula: C25H31N5O4
* Refer to Certificate of Analysis for lot specific data (including water content).
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AZD8055 is a selective ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM. AZD8055 inhibits the phosphorylation of mTORC1 substrates p70S6K and 4E-BP1 as well as phosphorylation of the mTORC2 substrate AKT and downstream proteins. AZD8055 fully inhibits the rapamycin-resistant T37/46 phosphorylation sites on 4E-BP1, resulting in significant inhibition of cap-dependent translation. AZD8055 inhibits proliferation and induces autophagy in H838 and A549 cells.

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO (93 mg/mL at 25 °C), water (<1 mg/mL at 25 °C), and ethanol (3 mg/mL at 25 °C).
Storage :
Store at -20° C
Melting Point :
204-208 °C
Boiling Point :
~694.30 °C at 760 mmHg
Density :
~1.2 g/cm3 (Predicted)
Refractive Index :
n20D 1.61 (Predicted)
IC50 :
mTOR (truncated): IC50 = 0.13 nM; mTOR (full length): IC50 = 0.8 nM; LU-139: IC50 = 23.31 nM (human); NCI-H720: IC50 = 23.98 nM (human); KARPAS-45: IC50 = 33.71 nM (human)
pK Values :
pKb: 6.48 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
25262965
MDL Number :
MFCD16660191
SMILES :
C[C@H]1COCCN1C2=NC(=NC3=C2C=CC(=N3)C4=CC(=C(C=C4)OC)CO)N5CCOC[C@@H]5C

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AZD8055  Product Citations

See how others have used AZD8055. Click on the entry to view the PubMed entry .

Citations 1 to 3 of 3 total

PMID: # 30595499  Villegas, F.|Lehalle, D.|Mayer, D.|Rittirsch, M.|Stadler, MB.|Zinner, M.|Olivieri, D.|Vabres, P.|Duplomb-Jego, L.|De Bont, ESJM.|Duffourd, Y.|Duijkers, F.|Avila, M.|Geneviève, D.|Houcinat, N.|Jouan, T.|Kuentz, P.|Lichtenbelt, KD.|Thauvin-Robinet, C.|St-Onge, J.|Thevenon, J.|van Gassen, KLI.|van Haelst, M.|van Koningsbruggen, S.|Hess, D.|Smallwood, SA.|Rivière, JB.|Faivre, L.|Betschinger, J.| et al. 2019. Cell Stem Cell. 24: 257-270.e8.

PMID: # 25893288  de Laurentiis, A. et al. 2015. Oncogene. 34: 6018-28.

PMID: # 24718556  Xie, S. et al. 2014. PLoS ONE. 9: e94496.

Citations 1 to 3 of 3 total
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Rated 5 out of 5 by from AZD8055 in plants We used the TOR inhibitor AZD8055 in the model plant Arabidopsis thaliana to activate autophagy, which perfectly works at a concentration of 1μm.
Date published: 2018-11-02
Rated 5 out of 5 by from Yang et al Yang et al. (PubMed ID 26221145) found that AZD8055 inhibited mammalian target rapamycin (mTOR) and induced cell death in hematopoietic stem and progenitor cells. -SCBT Publication Review
Date published: 2015-04-02
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