The Selective PI3K Inhibitor XL147 (SAR245408) Inhibits Tumor Growth and Survival and Potentiates the Activity of Chemotherapeutic Agents in Preclinical Tumor Models
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Abstract
Dysregulation of PI3K/PTEN pathway components, resulting in hyperactivated PI3K signaling, is frequently observed in various cancers and correlates with tumor growth and survival. Resistance to a variety of anticancer therapies, including receptor tyrosine kinase (RTK) inhibitors and chemotherapeutic agents, has been attributed to the absence or attenuation of downregulating signals along the PI3K/PTEN pathway. Thus, PI3K inhibitors have therapeutic potential as single agents and in combination with other therapies for a variety of cancer indications. XL147 (SAR245408) is a potent and highly selective inhibitor of class I PI3Ks (α, β, γ, and δ). Moreover, broad kinase selectivity profiling of >130 protein kinases revealed that XL147 is highly selective for class I PI3Ks over other kinases. In cellular assays, XL147 inhibits the formation of PIP3 in the membrane, and inhibits phosphorylation of AKT, p70S6K, and S6 in multiple tumor cell lines with diverse genetic alterations affecting the PI3K pathway. In a panel of tumor cell lines, XL147 inhibits proliferation with a wide range of potencies, with evidence of an impact of genotype on sensitivity. In mouse xenograft models, oral administration of XL147 results in dose-dependent inhibition of phosphorylation of AKT, p70S6K, and S6 with a duration of action of at least 24 hours. Repeat-dose administration of XL147 results in significant tumor growth inhibition in multiple human xenograft models in nude mice. Administration of XL147 in combination with chemotherapeutic agents results in antitumor activity in xenograft models that is enhanced over that observed with the corresponding single agents. Mol Cancer Ther; 14(4); 931–40. ©2015 AACR.
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XL147 was useful for PI3K mutation/amplification cell lines without KRAS/BRAF/PTEN mutation.
“Then, in an investigation of the effects of XL147 on proliferation in a panel of tumour cell lines, Shapiro et al. revealed that XL147 was useful for PI3K mutation/amplification cell lines without KRAS/BRAF/PTEN mutation [112].”
From Resistance to anti-EGFR therapies in metastatic colorectal cancer: underlying mechanisms and reversal strategies (2021) · cites this paper as [112]
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- Authors
- Foster, P., Yamaguchi, K., Hsu, P. P., Qian, F., Du, X., Wu, J., Won, K.-A., Yu, P., Jaeger, C. T., Zhang, W., Marlowe, C. K., Keast, P., Abulafia, W., Chen, J., Young, J., Plonowski, A., Yakes, F. M., Chu, F., Engell, K., Bentzien, F., Lam, S. T., Dale, S., Yturralde, O., Matthews, D. J., Lamb, P., & Laird, A. D.
- Affiliations
- Exelixis (United States) (US)
- Exelixis, Inc., South San Francisco, California.
- Corresponding author
- Laird, A. Douglas
- ORCID
- Venue
- Molecular Cancer Therapeutics
- Published
- 2015-04-01
- Volume
- 14
- Issue
- 4
- Pages
- 931-940
- ISSN
- 1535-7163 (ISSN-L)
- 1538-8514
- OpenAlex
- W1975685376
- Cited by
- 58
- References
- 29
- Citations by year
- 2026: 4 · 2025: 6 · 2024: 5 · 2023: 2 · 2022: 3 · 2021: 10 · 2020: 5 · 2019: 3 · 2018: 2 · 2017: 4 · 2016: 9 · 2015: 5
- FWCI
- 3.18
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Molecular Cancer Therapeutics (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Sanofi
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › PI3K/AKT/mTOR signaling in cancer
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Metabolism, Diabetes, and Cancer
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Advanced Breast Cancer Therapies
- Keywords
- PI3K inhibitors, class I PI3K, Akt phosphorylation, p70S6K, S6 phosphorylation, phosphatidylinositol 3,4,5-trisphosphate, chemosensitization, combination therapy, tumor growth inhibition, xenograft models, kinase selectivity, drug resistance
- MeSH terms
- Phosphoinositide-3 Kinase Inhibitors, Animals, Antineoplastic Agents, Cell Movement, Disease Models, Animal, Humans, Male, Mice, Nude, Neovascularization, Pathologic, Phosphorylation, Quinoxalines, Sulfonamides, Signal Transduction, Ribosomal Protein S6 Kinases, Xenograft Model Antitumor Assays, Cell Line, Tumor, Cell Proliferation, Proto-Oncogene Proteins c-akt, Mice
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