New “mTOR” inhibitor from Exelixis, Inc., XL 388

New Drug Approvals

XL 388

 A Novel Class of Highly Potent, Selective, ATP-Competitive, and Orally Bioavailable Inhibitors of the Mammalian Target of Rapamycin (mTOR)

Benzoxazepine-Containing Kinase Inhibitor

[7-(6-Aminopyridin-3-yl)-2,3-dihydro-1,4-benzoxazepin-4(5H)-yl][3-fluoro-2-methyl-4-(methylsulfonyl)phenyl]methanone
 [7-​(6-​amino-​3-​pyridinyl)​-​2,​3-​dihydro-​1,​4-​benzoxazepin-​4(5H)​-​yl]​[3-​fluoro-​2-​methyl-​4-​(methylsulfonyl)​phenyl]​-Methanone,
(7-(6-Aminopyridin-3-yl)-2,3-dihydrobenz[f][1,4]oxazepin-4(5H)-yl)(3-fluoro-2-methyl-4-(methylsulfonyl)phenyl)methanone
MW 455.50, CAS 1251156-08-7, MF C23 H22 F N3 O4 S
Exelixis, Inc. INNOVATOR, IND Filed
½H2O
C23H22FN3O4S.½H2O ,  Molecular Weight: 464.51
MONO HYDROCHLORIDE…..CAS 1777807-51-8, [7-(6-Aminopyridin-3-yl)-2,3-dihydro-1,4-benzoxazepin-4(5H)-yl][3-fluoro-2-methyl-4-(methylsulfonyl)phenyl]methanone Hydrochloride (1·HCl)
TLC Rf = 0.33 (Dichloromethane:Methanol [95:5])
Potent and selective mTOR inhibitor (IC50 = 9.9 nM). Inhibits mTOR activity in an ATP-competitive manner. Exhibits >300-fold selectivity for mTOR over PI 3-K and a range of other kinases. Displays antitumor activity in athymic nude mice implanted with tumor xenografts.
SYNTHESIS
 
 CLICK ON IMAGE FOR CLEAR VIEW……………..
 
Tyrosine kinases are important enzymes for signal transduction in cells. Therefore, they are often targets for the treatment of diseases that are caused by dysregulation…

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