An open source plant kinase chemogenomics set.
Ercoli MF, Ramos PZ, Jain R, Pilotte J, Dong OX, Thompson T, Wells CI, Elkins JM, Edwards AM, Couñago RM, Drewry DH, Ronald PC.
Plant Direct · research-article; journal article · DOI 10.1002/pld3.460 PUBLICATION REGISTRY
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Publikationer som ChEBI hänvisar till för CHIR-265. Visa hela publikationsregistret
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22 hitsSmall molecule RAF265 as an antiviral therapy acts against HSV-1 by regulating cytoskeleton rearrangement and cellular translation machinery.
Li CC, Chi XJ, Wang J, Potter AL, Wang XJ, Yang CJ.
J Med Virol · research support, non-u.s. gov't; journal article · DOI 10.1002/jmv.28226Small-Molecule RAF265 as an Antiviral Therapy Acts against PEDV Infection.
Wang J, Tian WJ, Li CC, Zhang XZ, Fan K, Li SL, Wang XJ.
Viruses · research support, non-u.s. gov't; research-article; journal article · DOI 10.3390/v14102261New tools for evaluating protein tyrosine sulfation: tyrosylprotein sulfotransferases (TPSTs) are novel targets for RAF protein kinase inhibitors.
Byrne DP, Li Y, Ngamlert P, Ramakrishnan K, Eyers CE, Wells C, Drewry DH, Zuercher WJ, Berry NG, Fernig DG, Eyers PA.
Biochem J · research support, non-u.s. gov't; research-article; journal article · DOI 10.1042/bcj20180266Therapeutic potential of combined BRAF/MEK blockade in BRAF-wild type preclinical tumor models.
Del Curatolo A, Conciatori F, Cesta Incani U, Bazzichetto C, Falcone I, Corbo V, D'Agosto S, Eramo A, Sette G, Sperduti I, De Luca T, Marabese M, Shirasawa S, De Maria R, Scarpa A, Broggini M, Del Bufalo D, Cognetti F, Milella M, Ciuffreda L.
J Exp Clin Cancer Res · research-article; journal article · DOI 10.1186/s13046-018-0820-5A first-in-human phase I, multicenter, open-label, dose-escalation study of the oral RAF/VEGFR-2 inhibitor (RAF265) in locally advanced or metastatic melanoma independent from BRAF mutation status.
Izar B, Sharfman W, Hodi FS, Lawrence D, Flaherty KT, Amaravadi R, Kim KB, Puzanov I, Sosman J, Dummer R, Goldinger SM, Lam L, Kakar S, Tang Z, Krieter O, McDermott DF, Atkins MB.
Cancer Med · clinical trial, phase ii; research-article; multicenter study; clinical trial, phase i; journal article · DOI 10.1002/cam4.1140Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.
Williams TE, Subramanian S, Verhagen J, McBride CM, Costales A, Sung L, Antonios-McCrea W, McKenna M, Louie AK, Ramurthy S, Levine B, Shafer CM, Machajewski T, Renhowe PA, Appleton BA, Amiri P, Chou J, Stuart D, Aardalen K, Poon D.
ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/ml500526pSynergistic antitumour activity of RAF265 and ZSTK474 on human TT medullary thyroid cancer cells.
Bertazza L, Barollo S, Radu CM, Cavedon E, Simioni P, Faggian D, Plebani M, Pelizzo MR, Rubin B, Boscaro M, Pezzani R, Mian C.
J Cell Mol Med · research support, non-u.s. gov't; research-article; journal article · DOI 10.1111/jcmm.12612Preclinical analysis of the anti-tumor and anti-metastatic effects of Raf265 on colon cancer cells and CD26(+) cancer stem cells in colorectal carcinoma.
Chow AK, Cheng NS, Lam CS, Ng L, Wong SK, Wan TM, Wan TM, Man JH, Cheung AH, Yau TC, Poon JT, Law WL, Pang RW.
Mol Cancer · retracted publication; research support, non-u.s. gov't; research-article; journal article · DOI 10.1186/s12943-015-0352-yTransient MEK inhibitor-associated retinopathy in metastatic melanoma.
Urner-Bloch U, Urner M, Stieger P, Galliker N, Winterton N, Zubel A, Moutouh-de Parseval L, Dummer R, Goldinger SM.
Ann Oncol · research support, non-u.s. gov't; journal article · DOI 10.1093/annonc/mdu169The combination of RAF265, SB590885, ZSTK474 on thyroid cancer cell lines deeply impact on proliferation and MAPK and PI3K/Akt signaling pathways.
Barollo S, Bertazza L, Baldini E, Ulisse S, Cavedon E, Boscaro M, Pezzani R, Mian C.
Invest New Drugs · research support, non-u.s. gov't; journal article · DOI 10.1007/s10637-014-0108-3RAF265, a dual BRAF and VEGFR2 inhibitor, prevents osteoclast formation and resorption. Therapeutic implications.
Garcia-Gomez A, Ocio EM, Pandiella A, San Miguel JF, Garayoa M.
Invest New Drugs · research support, non-u.s. gov't; journal article · DOI 10.1007/s10637-012-9845-3RAF265 inhibits the growth of advanced human melanoma tumors.
Su Y, Vilgelm AE, Kelley MC, Hawkins OE, Liu Y, Boyd KL, Kantrow S, Splittgerber RC, Short SP, Short SP, Sobolik T, Zaja-Milatovic S, Dahlman KB, Amiri KI, Jiang A, Lu P, Shyr Y, Stuart DD, Levy S, Sosman JA, Richmond A.
Clin Cancer Res · research support, non-u.s. gov't; research-article; research support, u.s. gov't, non-p.h.s.; journal article; research support, n.i.h., extramural · DOI 10.1158/1078-0432.ccr-11-1122CEP-32496: a novel orally active BRAF(V600E) inhibitor with selective cellular and in vivo antitumor activity.
James J, Ruggeri B, Armstrong RC, Rowbottom MW, Jones-Bolin S, Gunawardane RN, Dobrzanski P, Gardner MF, Zhao H, Cramer MD, Hunter K, Nepomuceno RR, Cheng M, Gitnick D, Yazdanian M, Insko DE, Ator MA, Apuy JL, Faraoni R, Dorsey BD, Williams M, Bhagwat SS, Holladay MW.
Mol Cancer Ther · journal article · DOI 10.1158/1535-7163.mct-11-0645Research highlights. Protein kinase D3 is the genetic sensitizer of RAF inhibitor RAF265 in melanoma cells.
Lucchetti C, Rizzolio F, Castronovo M, Toffoli G.
Pharmacogenomics · comment; journal article · DOI 10.2217/pgs.11.112Synergistic action of a RAF inhibitor and a dual PI3K/mTOR inhibitor in thyroid cancer.
Jin N, Jiang T, Rosen DM, Nelkin BD, Ball DW.
Clin Cancer Res · research-article; journal article; research support, n.i.h., extramural · DOI 10.1158/1078-0432.ccr-11-0933Mesenchymal stem cells and carcinoma-associated fibroblasts sensitize breast cancer cells in 3D cultures to kinase inhibitors.
Dittmer A, Fuchs A, Oerlecke I, Leyh B, Kaiser S, Martens JW, Lützkendorf J, Müller L, Dittmer J.
Int J Oncol · research support, non-u.s. gov't; journal article · DOI 10.3892/ijo.2011.1073Protein kinase D3 sensitizes RAF inhibitor RAF265 in melanoma cells by preventing reactivation of MAPK signaling.
Chen J, Shen Q, Labow M, Gaither LA.
Cancer Res · journal article · DOI 10.1158/0008-5472.can-10-3761The novel Raf inhibitor Raf265 decreases Bcl-2 levels and confers TRAIL-sensitivity to neuroendocrine tumour cells.
Zitzmann K, de Toni E, von Rüden J, Brand S, Göke B, Laubender RP, Auernhammer CJ.
Endocr Relat Cancer · research support, non-u.s. gov't; journal article · DOI 10.1530/erc-10-0108Use of DNA microarray and small animal positron emission tomography in preclinical drug evaluation of RAF265, a novel B-Raf/VEGFR-2 inhibitor.
Tseng JR, Stuart D, Aardalen K, Kaplan A, Aziz N, Hughes NP, Gambhir SS.
Neoplasia · research support, non-u.s. gov't; research-article; journal article; research support, n.i.h., extramural · DOI 10.1593/neo.101466Compensatory activation of Akt in response to mTOR and Raf inhibitors - a rationale for dual-targeted therapy approaches in neuroendocrine tumor disease.
Zitzmann K, Rüden Jv, Brand S, Göke B, Lichtl J, Spöttl G, Auernhammer CJ.
Cancer Lett · comparative study; research support, non-u.s. gov't; journal article · DOI 10.1016/j.canlet.2010.02.018Dependence on phosphoinositide 3-kinase and RAS-RAF pathways drive the activity of RAF265, a novel RAF/VEGFR2 inhibitor, and RAD001 (Everolimus) in combination.
Mordant P, Loriot Y, Leteur C, Calderaro J, Bourhis J, Wislez M, Soria JC, Deutsch E.
Mol Cancer Ther · research support, non-u.s. gov't; journal article · DOI 10.1158/1535-7163.mct-09-1014