AZD-8055 is a potent, selective, and orally bioavailable ATP-competitive inhibitor of mammalian target of rapamycin (mTOR) kinase activity, targeting both mTORC1 and mTORC2 complexes. It exhibits an IC₅₀ of 0.8 nM against mTOR in biochemical assays and demonstrates high selectivity over PI3K isoforms (IC₅₀ >10,000 nM for PI3Kα/β/δ/γ). In cellular assays, AZD-8055 effectively inhibits phosphorylation of downstream targets such as 4EBP1 and AKT (Ser473), with sub-nanomolar potency. It shows strong antiproliferative effects across a range of cancer cell lines, including breast, lung, and colorectal cancers, with GI₅₀ values typically in the low nanomolar range. In xenograft models, AZD-8055 achieves tumor growth inhibition or regression, correlating with suppression of mTOR signaling, and has been shown to induce apoptosis in some contexts.
MedKoo Cat#: 575210
Name: AZD-8055 fumarate
CAS#: 1201799-05-4 (fumarate)
Chemical Formula: C29H35N5O8
Exact Mass: 581.2486
Molecular Weight: 581.63
Elemental Analysis: C, 59.89; H, 6.07; N, 12.04; O, 22.01
The following data is based on the product molecular weight 581.63 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |