Content Links:

XL647

XL880

XL184

Related Publications

XL647

Ferrara N, Gerber HP, LeCouter J (2003). The biology of VEGF and its receptors. Nat. Med. 9, 669-676.
Ferrara N, Hillan KJ, Gerber HP, et al. (2004). Discovery and development of bevacizumab, an anti-VEGF antibody for treating cancer. Nat Rev Drug Discov. 3(5):391-400.
Gendreau SB, Ventura R, Keast P, et al. (2007). Inhibition of the T790M "Gatekeeper" Mutant of the Epidermal Growth Factor Receptor by EXEL-7647(XL647), a Novel Spectrum-Selective Kinase Inhibitor. Clin Canc Res. In press.
Mosesson Y, Yarden Y (2004). Oncogenic growth factor receptors: implications for signal transduction therapy. Semin Cancer Biol 14(4):262-70.
Normanno N, Bianco C, Strizzi L, et al. (2005). The ErbB receptors and their ligands in cancer: an overview. Curr Drug Targets 6(3):243-57.
Rizvi NA, Kris MG, Miller VA et al. (2007). A phase II study of XL647 in non-small cell lung cancer (NSCLC) patients enriched for presence of EGFR mutations. Seoul, South Korea. 12th World Conference on Lung Cancer; 2007. Abstract and Poster: XL647 IASLC (September 2007)
Sikic BI, Adjei, AA, Halsey J, et al. A phase I dose-escalation and pharmacokinetic (PK) study of a novel spectrum-selective kinase inhibitor, XL647, in patients with advanced solid malignancies (ASM). Prague, Czech Republic. 18th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics; 2006.
Poster: XL647 AACR-NCI-EORTC (November 2006)
Wakelee HA, Adjei AA, Halsey J, et al. (2006). A phase I dose-escalation and pharmacokinetic (PK) study of a novel spectrum selective kinase inhibitor, XL647, in patients with advanced solid malignancies (ASM). J Clin Oncol. 2006 ASCO Annual Meeting Proceedings Part I. Vol 24, No. 18S (June 20 Supplement), 2006:3044.
Poster: XL647 ASCO (June 2006)
Wakelee, HA, Adjei, AA, Keer H, et al. (2005). A phase I dose-escalation and pharmacokinetic (PK) study of a novel multiple-targeted receptor tyrosine kinase (RTK) inhibitor, XL647, in patients with advanced solid malignancies. J Clin Oncol 2005 ASCO Annual Meeting Proceedings. Vol 23, No. 16S, Part I of II (June 1 Supplement), 2005:3142.
Wakelee HA, Adjei AA, Halsey J, et al. A phase I dose-escalation and pharmacokinetic (PK) study of a novel spectrum selective kinase inhibitor (SSKI), XL647, in patients with advanced solid malignancies. Philadelphia, PA. 17th AACR-NCI-EORTC Symposium on Molecular Targets and Cancer Therapeutics; 2005.
Poster: XL647 AACR-NCI-EORTC (November 2005)

Back to XL647 Overview

XL880 / XL184

Birchmeier C, Birchmeier W, Gherardi E, et al. (2003). Met, metastasis, motility and more. Nat. Rev. Mol. Cell Biol. 4:915-25.
Boccaccio C, Comoglio PM (2006). Invasive growth: a MET-driven genetic programme for cancer and stem cells. Nat Rev Cancer. 6(8):637-45.
Bottaro DP, Liotta LA (2003). Cancer: Out of air is not out of action. Nature 423:593-5.
Christensen JG, Burrows J, Salgia R (2005). c-Met as a target for human cancer and characterization of inhibitors for therapeutic intervention. Cancer Lett. 225(1):1-26.
Corso, S, Comoglio, PM, Giordano S (2005). Cancer therapy: can the challenge be MET? Trends Mol Med. 11(6):284-92.
de Groot JW, Links TP, Plukker JT, et al. (2006). RET as a diagnostic and therapeutic target in sporadic and hereditary endocrine tumors. Endocr Rev. 27(5):535-60.
Eder JP, Appleman L, Heath E, et al. (2006). A phase I study of a novel spectrum selective kinase inhibitor (SSKI), XL880, administered orally in patients (pts) with advanced solid tumors (STs). J Clin Oncol. 2006 ASCO Annual Meeting Proceedings Part I. Vol 24, No. 18S (June 20 Supplement), 2006:3041.
Poster: XL880 ASCO (June 2006)
Joly AH. Simultaneous blockade of VEGF and HGF receptors results in potent anti-angiogenic and anti-tumor effects. Prague, Czech Republic. 18th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics; 2006.
LoRusso P, Appleman L, Heath E, et al. A phase I study of a novel spectrum selective kinase inhibitor (SSKI), XL880, administered orally in patients with advanced solid tumors. Philadelphia, PA. 17th AACR-NCI-EORTC Symposium on Molecular Targets and Cancer Therapeutics; 2005.
Poster: XL880 AACR-NCI-EORTC (November 2005)
LoRusso P, Appleman L, Zhu AX, et al. Pharmacodynamics of XL880, a novel spectrum selective kinase inhibitor (SSKI) administered orally in patients with advanced solid tumors (AST). Prague, Czech Republic. 18th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics; 2006.
Poster: XL880 AACR-NCI-EORTC (November 2006)
Razelle K, Camacho L, Hong D, et al. A phase 1 dose-escalation study of the safety and pharmacokinetics of XL184, a VEGFR and met kinase inhibitor, administered orally to subjects with advanced malignancies. Prague, Czech Republic. 18th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics; 2006.
Poster: XL184 AACR-NCI-EORTC (November 2006)

Back to XL880 Overview
Back to XL184 Overview

XL820

Carmeliet P (2005). VEGF as a key mediator of angiogenesis in cancer. Oncology. 69 Suppl 3:4-10.
Curtin JA, Busam K, Pinkel D, et al. (2006). Somatic activation of KIT in distinct subtypes of melanoma. J Clin Oncol. 24(26):4340-6.
Fletcher JA, Rubin BP (2007). KIT mutations in GIST. Curr Opin Genet Dev. 17(1):3-7.
Frohling S, Scholl C, Gilliland DG, et al. (2005). Genetics of myeloid malignancies: pathogenetic and clinical implications. J Clin Oncol, 23(26):6285-6295.
Heinrich MC, Blanke CD, Druker BJ, et al. (2002). Inhibition of KIT tyrosine kinase activity: a novel molecular approach to the treatment of KIT-positive malignancies. Journal of Clinical Oncology, 20:1692-1703.
Laird AD, Cherrington JM (2003). Small molecule tyrosine kinase inhibitors: clinical development of anticancer agents. Expert Opin Investig Drugs. 12(1):51-64.
Lennartsson J, Ronnstrand L (2006). The stem cell factor receptor/c-Kit as a drug target in cancer. Curr Cancer Drug Targets. 6(1):65-75.
Papadopoulos KP, Rodon J, Mita A, et al. A phase 1 dose-escalation study of the safety and pharmacokinetics of a novel spectrum selective kinase inhibitor, XL820, administered orally to patients with solid tumors. Prague, Czech Republic. 18th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics; 2006.
Poster: XL820 AACR-NCI-EORTC (November 2006)
Sattler M, Salgia R (2004). Targeting c-Kit mutations: basic science to novel therapies. Leuk Res, 28 Suppl 1:S11-20.

Back to XL820 Overview

XL844

Bartek J, Lukas J (2003). Chk1 and Chk2 kinases in checkpoint control and cancer. Cancer Cell 3(5):421-9.
Matthew DJ. Dissecting the roles of Chk1 and Chk2 in mitotic catastrophe using chemical genetics. Prague, Czech Republic. 18th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics; 2006.
Matthews DJ, Yakes FM, Chen J, et al. (2007). Pharmacological abrogation of S-phase checkpoint enhances the anti-tumor activity of gemcitabine in vivo. Cell Cycle. 6:104-10.
Zhou BB, Bartek J (2004). Targeting the checkpoint kinases: chemosensitization versus chemoprotection. Nat Rev Cancer 4(3):216-25.
Zhou BB, Sausville EA (2003). Drug discovery targeting Chk1 and Chk2 kinases. Prog Cell Cycle Res 5:413-21.

Back to XL844 Overview

XL999

Bergers G, Song S, Meyer-Morse N, et al. (2003). Benefits of targeting both pericytes and endothelial cells in the tumor vasculature with kinase inhibitors. J. Clin. Invest. 111:1287-1295.
Casanovas O, Hicklin DJ, Bergers G, et al. (2005). Drug resistance by evasion of antiangiogenic targeting of VEGF signaling in late-stage pancreatic islet tumors. Cancer Cell 8:299-309.
Cripe LD, Stadler WM, Wertheim M, et al. (2007). Integrated report of the phase 2 experience with XL999 administered IV to patients with non-small cell lung carcinoma (CA), renal cell CA, metastatic colorectal CA, recurrent ovarian CA, acute myelogenous leukemia, and multiple myeloma. Chicago, IL. 2007 ASCO Annual Meeting; 2007. Abstract and Poster: XL647 ASCO (June 2007).
Cross MJ, Claesson-Welsh L (2001). FGF and VEGF function in angiogenesis: signalling pathways, biological responses and therapeutic inhibition. Trends in Pharmacological Sciences 22:201-207.
Cooper J, Mita MM, Curtright J (2006). A phase I study examining weekly dosing and pharmacokinetics (PK) of a novel spectrum selective kinase inhibitor, XL999, in patients (pts) with advanced solid malignancies (ASM). J Clin Oncol. 2006 ASCO Annual Meeting Proceedings Part I. Vol 24, No. 18S (June 20 Supplement), 2006: 13024.
Ferrara N, Hillan KJ, Gerber HP, et al (2004). Discovery and development of bevacizumab, an anti-VEGF antibody for treating cancer. Nat Rev Drug Discov. 3(5):391-400.
Gilliland DG, Griffin JD (2002). Role of FLT3 in leukemia. Curr Opin Hematol. 9(4):274-81.
Krejci P, Mekikian PB, Wilcox WR (2006). The fibroblast growth factors in multiple myeloma. Leukemia. 20(6):1165-8.
Laird AD, Cherrington JM (2003). Small molecule tyrosine kinase inhibitors: clinical development of anticancer agents. Expert Opin Investig Drugs. 12(1):51-64.
Mita MM, Cooper J, Britt S, et al. A phase 1 study examining weekly weight-based or fixed dosing and pharmacokinetics of a novel spectrum selective kinase inhibitor, XL999, in patients with advanced solid malignancies. Prague, Czech Republic. 18th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics; 2006.
Poster: Poster: XL999 AACR-NCI-EORTC (November 2006)
Papadopoulos KP, Mita MM, Curtright J. A phase 1 dose-escalation and pharmaokinetic (PK) study of a novel spectrum selective kinase inhibitor (SSKI), XL999, in patients with advanced solid malignancies. Philadelphia, PA. 17th AACR-NCI-EORTC Symposium on Molecular Targets and Cancer Therapeutics; 2005.
Poster: XL999 AACR-NCI-EORTC (November 2005)
Pietras K, Sjoblom T, Rubin K, et al. (2003). PDGF receptors as cancer drug targets. Cancer Cell. 3(5):439-43.
Trudel S, Li ZH, Wei E, et al. (2005). CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma. Blood 105(7):2941-8.

Back to XL999 Overview

XL281

Beeram M, Patnaik A, Rowinsky EK (2005). Raf: a strategic target for therapeutic development against cancer. J Clin Oncol 23(27):6771-90.
Downward J (2003). Targeting RAS signaling pathways in cancer therapy. Nat. Rev Cancer 3:11-22.
Sebolt-Leopold JS, Herrera R (2004). Targeting the mitogen-activated protein kinase cascade to treat cancer. Nat Rev Cancer 4:937-94.
Nicoll M. Selective Inhibition of RAF results in downregulation of the RAS/RAF/MEK/ERK pathway and inhibition of tumor growth in vivo. Prague, Czech Republic. 18th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics; 2006.

Back to XL281 Overview

XL418

Hennessy BT, Smith DL, Ram PT, et al. (2005). Exploiting the PI3K/AKT pathway for cancer drug discovery. Nat Rev Drug Discov 4:988-1004.
Lamb P. Targeting aberrant PI-3 kinase pathway signaling by dual inhibition of AKT and p70S6K. Prague, Czech Republic. 18th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics; 2006.
Mamane Y, Petroulakis E, LeBacquer O, et al. (2006). mTOR, translation initiation and cancer. Oncogene. 25(48):6416-22.
Mitsiades CS, Mitsiades N, Koutsilieris M (2004). The Akt pathway: molecular targets for anti-cancer drug development. Curr Cancer Drug Targets 4:235-256.
Sansal I, Sellers WR (2004). The biology and clinical relevance of the PTEN tumor suppressor pathway. J Clin Oncol 22:2954-2963.

Back to XL418 Overview

XL228

Aftab DT. Simultaneous inhibition of IGF1R and SRC family kinases causes tumor growth inhibition and tumor regression in xenograft models. Prague, Czech Republic. 18th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics; 2006.
Mitsiades CS, Mitsiades NS, McMullan CJ, et al. (2004). Inhibition of the insulin-like growth factor receptor-1 tyrosine kinase activity as a therapeutic strategy for multiple myeloma, other hematologic malignancies, and solid tumors. Cancer Cell 5(3):221-30.
Parsons SJ, Parsons JT (2004). Src family kinases, key regulators of signal transduction. Oncogene 23:7906-9.
Pollak MN, Schernhammer ES, Hankinson SE (2004). Insulin-like growth factors and neoplasia. Nat Rev Cancer 4:505-18.
Shah NP, Sawyers CL (2003). Mechanisms of resistance to STI571 in Philadelphia chromosome-associated leukemias. Oncogene 22(47):7389-7395.
Weisberg E, Manley PW, Cowan-Jacob SW, et al. (2007). Second generation inhibitors of BCR-ABL for the treatment of imatinib-resistant chronic myeloid leukaemia. Nat Rev Cancer 7(5):345-56.
Yeatman TJ (2004). A renaissance for SRC Nat Rev Cancer 4(6):470-80.
Yee D (2006). Targeting insulin-like growth factor pathways. Br J Cancer 94(4):465-8.
Zhang W. Inhibition of the drug-resistant T315I mutant of BCR-ABL. Prague, Czech Republic. 18th EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics; 2006.

Back to XL228 Overview

XL518

Kohno M, Pouyssegur J (2006). Targeting the ERK signaling pathway in cancer therapy. Ann Med. 38(3):200-11.

Back to XL518 Overview

XL147

Cully M, You H, Levine AJ, et al. (2006). Beyond PTEN mutations: the PI3K pathway as an integrator of multiple inputs during tumorigenesis. Nat Rev Cancer 6(3):184-92.

Back to XL147 Overview

XL765

Arsham AM, Neufeld TP (2006). Thinking globally and acting locally with TOR. Curr Opin Cell Biol. 18(6):589-97.
Cully M, You H, Levine AJ, et al. (2006). Beyond PTEN mutations: the PI3K pathway as an integrator of multiple inputs during tumorigenesis. Nat Rev Cancer 6(3):184-92.
Easton JB, Houghton PJ, (2006). mTOR and cancer therapy. Oncogene 25(48):6436-46.

Back to XL765 Overview

XL019

Ahmed A, Chang C-C (2006). Chronic Idiopathic Myelofibrosis, Clinicopathologic Features, Pathogenesis, and Prognosis. Arch Pathol Lab Med. 130:1133-43.
Barton BE, Karras, JG, Murphy TF, et al. (2004). Signal transducer and activator of transcription 3 (STAT3) activation in prostate cancer: Direct STAT3 inhibition induces apoptosis in prostate cancer lines. Mol Cancer Ther. 3:11-20.
Flowers LO, Subramaniam PS, Johnson HM (2005). A SOCS-1 peptide mimetic inhibits both constitutive and IL-6 induced activation of STAT3 in prostate cancer cells. Oncogene 24:2114-2120.
Fujimoto M, Naka T (2003). Regulation of cytokine signaling by SOCS family molecules.Trends Immunol. 24(12):659-66.
Haura EB, Turkson J, Jove R (2005). Mechanisms of disease: Insights into the emerging role of signal transducers and activators of transcription in cancer. Nat Clin Pract Oncol. 2(6):315-24.
Ihle JN, Gilliland DG (2007). Jak2: normal function and role in hematopoietic disorders. Curr Opin Genet Dev. 17(1):8-14.
Levine RL, Gilliland DG (2007). JAK-2 mutations and their relevance to myeloproliferative disease. Curr Opin Hematol. 14(1):43-7.
Renne C, Willenbrock K, Martin-Subero JI, et al. (2007). High expression of several tyrosine kinases and activation of the PI3K/AKT pathway in mediastinal large B cell lymphoma reveals further similarities to Hodgkin lymphoma. Leukemia 21(4):780-7.
Tefferi A, Gilliland DG (2005). JAK2 in myeloproliferative disorders is not just another kinase. Cell Cycle 4:1053-1056.
Wernig G, Mercher T, Okabe R, et al. (2006). Expression of Jak2 V617F causes a polycythemia vera-like disease with associated myelofibrosis in a murine bone marrow transplant model. Blood 107:4274-81.
Yasuda Y, Fujita Y, Matsuo T, et al. (2003). Erythropoietin regulates tumour growth of human malignancies. Carcinogenesis 24:1021-1029.

Back to XL019 Overview