270902-51-7
Chemical Structure
LAF389
- CAS No.: 270902-51-7
- Formula:C25H42N2O8
- Molecular Weight:498.61
IUPAC Name: (3R,6S)-7-oxo-6-((2R,3R,4S,5R,E)-3,4,5-trihydroxy-2-methoxy-8,8-dimethylnon-6-enamido)azepan-3-yl cyclohexanecarboxylate
InChIKey: XSYJUVKQRPLTAU-BKMGADMVSA-N
SMILES: CC(C)(C)/C=C/[C@@H](O)[C@H](O)[C@@H](O)[C@@H](OC)C(N[C@H]1CC[C@H](CNC1=O)OC(C2CCCCC2)=O)=O
Biological Activity: LAF389, a prodrug of LAF153 (HY-183876), is a methionine aminopeptidase (MetAps) inhibitor with an IC50 of 800 nM against MetAp2, and exhibits a maximum inhibition rate of 20% against MetAp1 at 300 nM. LAF389 possesses antiproliferative, antiangiogenic and cytotoxic activities. LAF389 can be used in research related to cancers such as advanced solid tumors[1][2].
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LAF389 | LAF389, a prodrug of LAF153 (HY-183876), is a methionine aminopeptidase (MetAps) inhibitor with an IC50 of 800 nM against MetAp2, and exhibits a maximum inhibition rate of 20% against MetAp1 at 300 nM. LAF389 possesses antiproliferative, antiangiogenic and cytotoxic activities. LAF389 can be used in research related to cancers such as advanced solid tumors. | |||||||||||||||||||||
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References
- [1]. Dumez H, et al. A phase I and pharmacokinetic study of LAF389 administered to patients with advanced cancer. Anticancer Drugs. 2007;18(2):219-225. [Content Brief]
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[2]. Towbin H, et al. Proteomics-based target identification: bengamides as a new class of methionine aminopeptidase inhibitors. Journal of Biological Chemistry. 2003 Dec 26;278(52):52964-71.
