AZD8055 Inhibitor CAS No. 1009298-09-2

Cat. No.	Name	Size	Price	Add Cart
KI0445	AZD8055	10 mg	$192
KI0445	AZD8055	50 mg	$330

Chemical Characteristic

Product Name	AZD8055
CAS No.	1009298-09-2
Molecular Weight	465.54
Formula	C₂₅H₃₁N₅O₄
Chemical Name	(5-(2,4-bis((S)-3-methylmorpholino)pyrido[2,3-d]pyrimidin-7-yl)-2-methoxyphenyl)methanol
Smiles	C(O)c1c(ccc(c1)c1ccc2c(nc(nc2N2[C@@H](COCC2)C)N2[C@@H](COCC2)C)n1)OC
Chemical Structure

Biological activities

AZD8055 is a novel ATP-competitive inhibitor of mTOR kinase activity. The IC50 of AZD8055 is 0.8 nM. AZD8055 displays potent selectivity (∼1,000-fold) against not only all class I phosphatidylinositol 3-kinase (PI3K) isoforms but also other members of the PI3K-like kinase family. AZD8055 inhibits the phosphorylation of mTORC1 substrates p70S6K and 4E-BP1. Additionally, AZD8055 also prevents the phosphorylation of the mTORC2 substrate AKT and downstream proteins. The rapamycin-resistant T37/46 phosphorylation sites on 4E-BP1 are completely inhibited by AZD8055, leading to significant prevention of cap-dependent translation. AZD8055 potently suppresses proliferation and induces autophagy in H838 and A549 cells. The IC50 for AZD8055 against truncated recombinant mTOR enzyme is 0.13 nM. AZD8055 inhibits the native mTOR enzyme complexes extracted from HeLa cells with an IC50 of 0.8 nM. The Ki for AZD8055 is demonstrated to be 1.3 nM. AZD8055 is counterscreened against the most closely related kinases, class I and class III PI3K lipid kinases and the PIKK family members ATM and DNA-PK, where it reveals at least a 1,000-fold differential in potency. In cellular levels, IC50s for AZD8055 is 24 nM for pAKT Ser⁴⁷³ and 27 nM for pS6 Ser^235/236. 5 nM AZD8055 inhibits p70S6K by 70% to 80% in MCF-7 and HEK cells. AZD8055 concentration-dependently decreases pPRAS40 T246 with a maximum inhibition of 70% to 95% in HEK293, U87-MG (PTEN null), A549 (Kras and LKB1 mutant). In mice bearing U87-MG (PTEN null) glioblastoma xenografts, oral treatment with AZD8055 dose-dependently inhibits tumor growth by 33%, 48%, and 77% with 2.5, 5, and 10 mg/kg/d twice daily, respectively. The prevention of pAKT is more than 50% for at least 8 hours in animals receiving the dose of 10 mg/kg AZD8055. ^[1]

Protocols

AZD8055 is prepared as 10 mM stock solution in DMSO and stored under nitrogen. ^[1]

References

[1] Chresta CM, et al. 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. 2010, 70(1): 288-298.

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