PQR309 Is a Novel Dual PI3K/mTOR Inhibitor with Preclinical Antitumor Activity in Lymphomas as a Single Agent and in Combination Therapy

No abstract is available for this paper.

• Publication year

  2017

• Venue

  Clinical Cancer Research

• Publication date

  2017-10-24

• Fields of study

  Medicine

• Identifiers
  DOI 10.1158/1078-0432.CCR-17-1041PMID 29066507
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

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  2016influential reference
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  2015influential reference
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