Identification of Novel, Selective Ataxia-Telangiectasia Mutated Kinase Inhibitors with the Ability to Penetrate the Blood–Brain Barrier: The Discovery of AZD1390
Pike, Kurt G., Hunt, Thomas A., Barlaam, Bernard, Benstead, David, Cadogan, Elaine, Chen, Kan, Cook, Calum R., Colclough, Nicola, Deng, Chao, Durant, Stephen T., Eatherton, Andrew, Goldberg, Kristin, Johnström, Peter, Liu, Libin, Liu, Zhaoqun, Nissink, J. Willem M., Pang, Chengling, Pass, Martin, Robb, Graeme R., Roberts, Caroline, Schou, Magnus, Steward, Oliver, Sykes, Andy, Yan, Yumei, Zhai, Baochang, Zheng, Li
Published in Journal of medicinal chemistry (22.02.2024)
Published in Journal of medicinal chemistry (22.02.2024)
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Abstract 6168: Characterization of ATM inhibitor (AZD1390) distribution and pharmacodynamic changes in brain and glioblastoma in preclinical models to inform on mechanism of action
Oplustil O'Connor, Lenka, Hamm, Gregory, Udriste, Maria, Ling, Stephanie, Wilson, Joanne, Durant, Steve, Hughes, Gareth, Cosulich, Sabina, Shao, Wenlin, Pass, Martin, Jones, Gemma, Pierce, Andrew, Goodwin, Richard, O'Connor, Mark, Barrett, Carl, Harrington, Elizabeth
Published in Cancer research (Chicago, Ill.) (15.08.2020)
Published in Cancer research (Chicago, Ill.) (15.08.2020)
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Orally Bioavailable and Blood-Brain Barrier-Penetrating ATM Inhibitor (AZ32) Radiosensitizes Intracranial Gliomas in Mice
Karlin, Jeremy, Allen, Jasmine, Ahmad, Syed F, Hughes, Gareth, Sheridan, Victoria, Odedra, Rajesh, Farrington, Paul, Cadogan, Elaine B, Riches, Lucy C, Garcia-Trinidad, Antonio, Thomason, Andrew G, Patel, Bhavika, Vincent, Jennifer, Lau, Alan, Pike, Kurt G, Hunt, Thomas A, Sule, Amrita, Valerie, Nicholas C K, Biddlestone-Thorpe, Laura, Kahn, Jenna, Beckta, Jason M, Mukhopadhyay, Nitai, Barlaam, Bernard, Degorce, Sebastien L, Kettle, Jason, Colclough, Nicola, Wilson, Joanne, Smith, Aaron, Barrett, Ian P, Zheng, Li, Zhang, Tianwei, Wang, Yingchun, Chen, Kan, Pass, Martin, Durant, Stephen T, Valerie, Kristoffer
Published in Molecular cancer therapeutics (01.08.2018)
Published in Molecular cancer therapeutics (01.08.2018)
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Capivasertib, an AKT Kinase Inhibitor, as Monotherapy or in Combination With Fulvestrant in Patients With AKT1E17K-Mutant, ER-Positive Metastatic Breast Cancer
Smyth, Lillian M., Tamura, Kenji, Oliveira, Mafalda, Ciruelos, Eva, Mayer, Ingrid A., Sablin, Marie-Paule, Biganzoli, Laura, Ambrose, Helen, Ashton, Jack, Barnicle, Alan, Cashell, Des, Corcoran, Claire, de Bruin, Elza C., Foxley, Andrew, Hauser, Joana, Lindemann, Justin P.O., Maudsley, Rhiannon, McEwen, Robert, Moschetta, Michele, Pass, Martin, Rowlands, Vicky, Schiavon, Gaia, Banerji, Udai, Scaltriti, Maurizio, Taylor, Barry S., Chandarlapaty, Sarat, Baselga, José, Hyman, David M.
Published in Clinical cancer research (20.04.2020)
Published in Clinical cancer research (20.04.2020)
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Discovery of a Potent, Selective, Orally Bioavailable, and Efficacious Novel 2‑(Pyrazol-4-ylamino)-pyrimidine Inhibitor of the Insulin-like Growth Factor‑1 Receptor (IGF-1R)
Degorce, Sébastien L, Boyd, Scott, Curwen, Jon O, Ducray, Richard, Halsall, Christopher T, Jones, Clifford D, Lach, Franck, Lenz, Eva M, Pass, Martin, Pass, Sarah, Trigwell, Catherine
Published in Journal of medicinal chemistry (26.05.2016)
Published in Journal of medicinal chemistry (26.05.2016)
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Novel imidazo[1,2-a]pyridine based inhibitors of the IGF-1 receptor tyrosine kinase: Optimization of the aniline
Ducray, Richard, Jones, Clifford D., Jung, Frederic H., Simpson, Iain, Curwen, Jon, Pass, Martin
Published in Bioorganic & medicinal chemistry letters (15.08.2011)
Published in Bioorganic & medicinal chemistry letters (15.08.2011)
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Journal Article
Capivasertib, an AKT Kinase Inhibitor, as Monotherapy or in Combination with Fulvestrant in Patients with AKT1 E17K -Mutant, ER-Positive Metastatic Breast Cancer
Smyth, Lillian M, Tamura, Kenji, Oliveira, Mafalda, Ciruelos, Eva M, Mayer, Ingrid A, Sablin, Marie-Paule, Biganzoli, Laura, Ambrose, Helen J, Ashton, Jack, Barnicle, Alan, Cashell, Des D, Corcoran, Claire, de Bruin, Elza C, Foxley, Andrew, Hauser, Joana, Lindemann, Justin P O, Maudsley, Rhiannon, McEwen, Robert, Moschetta, Michele, Pass, Martin, Rowlands, Vicky, Schiavon, Gaia, Banerji, Udai, Scaltriti, Maurizio, Taylor, Barry S, Chandarlapaty, Sarat, Baselga, José, Hyman, David M
Published in Clinical cancer research (01.08.2020)
Published in Clinical cancer research (01.08.2020)
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Journal Article
Discovery of a Series of 3‑Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors
Barlaam, Bernard, Cadogan, Elaine, Campbell, Andrew, Colclough, Nicola, Dishington, Allan, Durant, Stephen, Goldberg, Kristin, Hassall, Lorraine A, Hughes, Gareth D, MacFaul, Philip A, McGuire, Thomas M, Pass, Martin, Patel, Anil, Pearson, Stuart, Petersen, Jens, Pike, Kurt G, Robb, Graeme, Stratton, Natalie, Xin, Guohong, Zhai, Baochang
Published in ACS medicinal chemistry letters (09.08.2018)
Published in ACS medicinal chemistry letters (09.08.2018)
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Abstract A094: Phase I modular study of AZD0156, a first-in-class oral selective inhibitor of ataxia telangiectasia mutated protein kinase (ATM), in combination with olaparib (AToM Study, Module 1)
Abida, Wassim, Bang, Yung J., Carter, Louise, Azaro, Analía, Krebs, Matthew, Im, Seock-Ah, Chen, Yingxue, Buil-Bruna, Núria, Li, Yan, Eaton, David, Stephens, Christine, Ross, Graham, Pass, Martin, Rodon, Jordi, Dean, Emma
Published in Molecular cancer therapeutics (01.01.2018)
Published in Molecular cancer therapeutics (01.01.2018)
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Discovery of AZD3147: A Potent, Selective Dual Inhibitor of mTORC1 and mTORC2
Pike, Kurt G, Morris, Jeff, Ruston, Linette, Pass, Sarah L, Greenwood, Ryan, Williams, Emma J, Demeritt, Julie, Culshaw, Janet D, Gill, Kristy, Pass, Martin, Finlay, M. Raymond V, Good, Catherine J, Roberts, Craig A, Currie, Gordon S, Blades, Kevin, Eden, Jonathan M, Pearson, Stuart E
Published in Journal of medicinal chemistry (12.03.2015)
Published in Journal of medicinal chemistry (12.03.2015)
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The discovery and optimisation of pyrido[2,3- d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase
Malagu, Karine, Duggan, Heather, Menear, Keith, Hummersone, Marc, Gomez, Sylvie, Bailey, Christine, Edwards, Peter, Drzewiecki, Jan, Leroux, Frédéric, Quesada, Mar Jimenez, Hermann, Gesine, Maine, Stephanie, Molyneaux, Carrie-Anne, Le Gall, Armelle, Pullen, James, Hickson, Ian, Smith, Lisa, Maguire, Sharon, Martin, Niall, Smith, Graeme, Pass, Martin
Published in Bioorganic & medicinal chemistry letters (15.10.2009)
Published in Bioorganic & medicinal chemistry letters (15.10.2009)
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Journal Article
Abstract A104: AZD1390, a potent and selective orally bioavailable blood-brain barrier-penetrant ATM inhibitor, radiosensitizes and improves survival of orthotopic glioma and metastatic brain tumor models
Durant, Steve T., Pike, Kurt G., Colclough, Nicola, Riches, Lucy, Garcia-Trinidad, Antonio, Hunt, Thomas, Ling, Stephanie, Stott, Jonathan, Barrett, Ian, Zheng, Li, Wang, Yingchun, Chen, Kan, Zhang, Tianwei, Pilla Reddy, Venkatesh, Sykes, Andrew, Johnstrom, Peter, Jones, Gemma, Pierce, Andrew, Karlin, Jeremy, Kahn, Jenna, Allen, Jasmine, Valerie, Kristoffer, Illingworth, Ruth, Pass, Martin
Published in Molecular cancer therapeutics (01.01.2018)
Published in Molecular cancer therapeutics (01.01.2018)
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Discovery of 4‑Amino‑N‑[(1S)‑1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H‑pyrrolo[2,3‑d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an Orally Bioavailable, Potent Inhibitor of Akt Kinases
Addie, Matt, Ballard, Peter, Buttar, David, Crafter, Claire, Currie, Gordon, Davies, Barry R, Debreczeni, Judit, Dry, Hannah, Dudley, Philippa, Greenwood, Ryan, Johnson, Paul D, Kettle, Jason G, Lane, Clare, Lamont, Gillian, Leach, Andrew, Luke, Richard W. A, Morris, Jeff, Ogilvie, Donald, Page, Ken, Pass, Martin, Pearson, Stuart, Ruston, Linette
Published in Journal of medicinal chemistry (14.03.2013)
Published in Journal of medicinal chemistry (14.03.2013)
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Abstract 3041: Blood-brain barrier penetrating ATM inhibitor (AZ32) radiosensitises intracranial gliomas in mice
Durant, Steve T., Karlin, Jeremy, Pike, Kurt, Colclough, Nicola, Mukhopadhyay, N, Ahmad, S F., Bekta, J M., Tokarz, M, Bardelle, Catherine, Hughes, Gareth, Patel, Bhavika, Thomason, Andrew, Cadogan, Elaine, Barrett, Ian, Lau, Alan, Pass, Martin, Valerie, Kristoffer
Published in Cancer research (Chicago, Ill.) (15.07.2016)
Published in Cancer research (Chicago, Ill.) (15.07.2016)
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Abstract CT010: Phase I trial combining the PARP inhibitor olaparib (Ola) and AKT inhibitor AZD5363 (AZD) in germline (g)BRCA and non-BRCA mutant (m) advanced cancer patients (pts) incorporating noninvasive monitoring of cancer mutations
Michalarea, Vasiliki, Roda, Desam, Drew, Yvette, Carreira, Suzanne, O’Carrigan, Brent S., Shaw, Heather, Roux, Rene, Kumar, Sanjeev, Ward, Sarah, Parmar, Mona, Turner, Alison, Hall, Emma, Serrano Fandos, Sonia, Perez, Raquel, Tunariu, Nina, Raynaud, Florence, Cullberg, Marie, Foxley, Andrew, Lindemann, Justin PO, Pass, Martin, Rugman, Paul, Lopez, Juanita S., Banerji, Udai, Basu, Bristi, Plummer, Ruth, Kristeleit, Rebecca, de Bono, Johann S., Yap, Timothy A.
Published in Cancer research (Chicago, Ill.) (15.07.2016)
Published in Cancer research (Chicago, Ill.) (15.07.2016)
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Abstract B109: AZD5363, a catalytic pan-Akt inhibitor, in Akt1 E17K mutation positive advanced solid tumors
Hyman, David M., Smyth, Lillian, Bedard, Philippe L., Oza, Amit, Dean, Emma, Armstrong, Anne, Lima, Joao, Bando, Hideaki, Kabos, Peter, Perez-Fidalgo, J. Alejandro, Moore, Kathleen, Westin, Shannon N., You, Benoit, Chandarlapaty, Sarat, Alland, Leila, Ambrose, Helen, Foxley, Andrew, Lindemann, Justin, Pass, Martin, Rugman, Paul, Salim, Shaista, Schiavon, Gaia, Tamura, Kenji, Baselga, Jose, Banerji, Udai
Published in Molecular cancer therapeutics (01.12.2015)
Published in Molecular cancer therapeutics (01.12.2015)
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Synthesis and evaluation of triazolones as checkpoint kinase 1 inhibitors
Oza, Vibha, Ashwell, Susan, Brassil, Patrick, Breed, Jason, Ezhuthachan, Jaychandran, Deng, Chun, Grondine, Michael, Horn, Candice, Liu, DongFang, Lyne, Paul, Newcombe, Nicholas, Pass, Martin, Read, Jon, Su, Mei, Toader, Dorin, Yu, Dingwei, Yu, Yan, Zabludoff, Sonya
Published in Bioorganic & medicinal chemistry letters (15.03.2012)
Published in Bioorganic & medicinal chemistry letters (15.03.2012)
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Journal Article
Pharmacodynamic activity of the AKT inhibitor AZD5363 in patients with advanced solid tumors
Elvin, Paul, Palmer, Amy, Womack, Chris, Tall, Matthew, Swales, Karen E, Garrett, Michelle D, Banerji, Udai, Tamura, Kenji, Cheung, S Y Amy, Lawrence, Peter, Lindemann, Justin, Ambrose, Helen, Stephens, Christine, Davies, Barry, Foxley, Andrew, Pass, Martin, Harrington, Elizabeth A., Barrett, J. Carl
Published in Journal of clinical oncology (20.05.2014)
Published in Journal of clinical oncology (20.05.2014)
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Abstract B238: Novel imidazo[1,2- a ]pyridines as inhibitors of the IGF-1R tyrosine kinase
Ducray, Richard, Simpson, Iain, Jones, Clifford D., Curwen, Jon, Trigwell, Catherine B., Veldman-Jones, Margaret H., Fitzek, Martina, Walker, Graeme E., Ward, Lara T., Hudson, Kevin, Pass, Martin
Published in Molecular cancer therapeutics (12.11.2011)
Published in Molecular cancer therapeutics (12.11.2011)
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Abstract 917: AZD2014, a dual mTORC1 and mTORC2 inhibitor is differentiated from allosteric inhibitors of mTORC1 in ER+ breast cancer
Guichard, Sylvie M., Howard, Zoe, Heathcote, Dan, Roth, Mark, Hughes, Gareth, Curwen, Jon, Yates, James, Logie, Armelle, Holt, Sarah, Chresta, Christine M., Davies, Barry R., Malagu, Karine, Hummersone, Marc, Pass, Sarah L., Green, Stephen, Pass, Martin
Published in Cancer research (Chicago, Ill.) (15.04.2012)
Published in Cancer research (Chicago, Ill.) (15.04.2012)
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