Cat. No. Name Size Price Add Cart
KI3049AP-23573 (MK-8669)5 mg$112
AP-23573 (MK-8669)10 mg$192
AP-23573 (MK-8669)20 mg$308
AP-23573 (MK-8669)50 mg$592
AP-23573 (MK-8669)1 g$4928

Chemical Characteristic

Product NameAP-23573 (MK-8669)
SynonymsDeforolimus
CAS No.572924-54-0
Molecular Weight 990.21
FormulaC53H84NO14P
Chemical Name42-?(dimethylphosphinate?)-rapamycin
Smiles[C@H]1(C[C@@H](CC[C@H]1OP(=O)(C)C)C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@@]2(O)[C@@H](CC[C@H](O2)C[C@@H](/C(=C/C=C/C=C/[C@H](C[C@H](C(=O)[C@@H]([C@@H](/C(=C/[C@H](C(=O)C1)C)/C)O)OC)C)C)/C)OC)C)OC
Chemical Structure

Biological activities

AP23573 is a novel mammalian target of rapmycin (mTOR) inhibitor. AP23573 inhibits mTOR signaling in tumors, leading to cell cycle arrest, tumor cell shrinkage and inhibition of angiogenesis. AP23573 potently inhibits the proliferation of human-derived tumor cell lines in vitro.[1] In vitro, AP23573 potently blocks mTOR activity and inhibits proliferation in multiple tumor cell lines, including an erythroleukemic line. AP23573 has shown activity against a broad range of human tumor xenografts using intermittent dosing schedules.[2]

References

[1] Rivera VM, et al. Anti-proliferative activity of the mTOR inhibitor AP23573 in combination with cytotoxic and targeted agents. Proc Amer Assoc Cancer Res. 2004, 45
[2] Rizzieri DA, et al. A phase 2 clinical trial of deforolimus (AP23573, MK-8669), a novel mammalian target of rapamycin inhibitor, in patients with relapsed or refractory hematologic malignancies. Clin Cancer Res. 2008, 14 (9): 2756-2762.

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