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

 

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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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Why I Joined Shoolini University?

Robins1987's Blog

Placed between two bustling cities of Chandigarh and Shimla, Shoolini University lies at the foothills of the Himalayas. Combining three academic fields of the future–science, technology and management, Shoolini University is a place for young aspirants who want to shape the future of their field of interest.

What makes Shoolini a favourite among students?

* This is the First Biotech University of India.
* Shoolini has a lush campus with pleasant weather round the year because it lies in a valley. You will often find snow capped peaks surrounding the campus.
* This is a fully wi-fi campus with a 2 mbps leased line.
* Each year the University takes interested students on an educative and entertaining tour in India or abroad.
* Shoolini institute SILB has consistently ranked among the top 15 private bio-tech institutes in India according to BioSpectrum Bioitech Schools Surveys.
* SU has an MOU with…

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