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Ganetespib, Rigosertib sodium, Niraparib


Name (nom): Ganetespib
Code name (nom de code): STA-9090
Type: synthetic small molecule (petite molecule synthétique)
Target (cible) : Hsp90

References :

Multifaceted intervention by the Hsp90 inhibitor ganetespib (STA-9090)
in cancer cells with activated JAK/STAT signaling. Proia DA, Foley KP,
Korbut T, Sang J, Smith D, Bates RC, Liu Y, Rosenberg AF, Zhou D, Koya
K, Barsoum J, Blackman RK. PLoS One. 2011 Apr 14;6(4):e18552.

STA-9090, a small-molecule Hsp90 inhibitor for the potential treatment
of cancer. Wang Y, Trepel JB, Neckers LM, Giaccone G. Curr Opin
Investig Drugs. 2010 Dec;11(12):1466-76.

Heat shock protein 90 regulates the expression of Wilms tumor 1
protein in myeloid leukemias. Bansal H, Bansal S, Rao M, Foley KP,
Sang J, Proia DA, Blackman RK, Ying W, Barsoum J, Baer MR, Kelly K,
Swords R, Tomlinson GE, Battiwalla M, Giles FJ, Lee KP, Padmanabhan S.
Blood. 2010 Nov 25;116(22):4591-9.

The novel HSP90 inhibitor STA-1474 exhibits biologic activity against
osteosarcoma cell lines. McCleese JK, Bear MD, Fossey SL, Mihalek RM,
Foley KP, Ying W, Barsoum J, London CA. Int J Cancer. 2009 Dec
15;125(12):2792-801.

The novel HSP90 inhibitor STA-9090 exhibits activity against Kit-
dependent and -independent malignant mast cell tumors. Lin TY, Bear M,
Du Z, Foley KP, Ying W, Barsoum J, London C. Exp Hematol. 2008 Oct;
36(10):1266-77.

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Name (nom): Rigosertib sodium
Code name (nom de code): ON 01910.Na
Otherl name : Estybon
Type: synthetic small molecule (petite molecule synthétique)
Target (cible) : polo-like kinase

References:

Discovery of a Clinical Stage Multi-Kinase Inhibitor Sodium (E)-2-{2-
Methoxy-5-[(2',4',6'-trimethoxystyrylsulfonyl)methyl]phenylamino}
acetate (ON 01910.Na): Synthesis, Structure-Activity Relationship, and
Biological Activity. Reddy MV, Venkatapuram P, Mallireddigari MR,
Pallela VR, Cosenza SC, Robell KA, Akula B, Hoffman BS, Reddy EP. J
Med Chem. 2011 Aug 17.

Polo-like kinase (PLK) inhibitors in preclinical and early clinical
development in oncology. Schöffski P. Oncologist. 2009 Jun;14(6):
559-70.

Evaluation of the novel mitotic modulator ON 01910.Na in pancreatic
cancer and preclinical development of an ex vivo predictive assay.
Jimeno A, Chan A, Cusatis G, Zhang X, Wheelhouse J, Solomon A, Chan F,
Zhao M, Cosenza SC, Ramana Reddy MV, Rudek MA, Kulesza P, Donehower
RC, Reddy EP, Hidalgo M. Oncogene. 2009 Jan 29;28(4):610-8.
4.

Phase I study of ON 01910.Na, a novel modulator of the Polo-like
kinase 1 pathway, in adult patients with solid tumors. Jimeno A, Li J,
Messersmith WA, Laheru D, Rudek MA, Maniar M, Hidalgo M, Baker SD,
Donehower RC. J Clin Oncol. 2008 Dec 1;26(34):5504-10.

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Name (nom): Niraparib
Code name (nom de code): MK4827 or MK-4827
Type: synthetic small molecule (petite molecule synthétique)
Target (cible) : Poly(ADP-ribose) polymerase (PARP)

References:

Small-molecule PARP modulators--current status and future therapeutic
potential. Penning TD. Curr Opin Drug Discov Devel. 2010 Sep;13(5):
577-86.

Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-
carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP)
inhibitor efficacious in BRCA-1 and -2 mutant tumors. Jones P,
Altamura S, Boueres J, Ferrigno F, Fonsi M, Giomini C, Lamartina S,
Monteagudo E, Ontoria JM, Orsale MV, Palumbi MC, Pesci S, Roscilli G,
Scarpelli R, Schultz-Fademrecht C, Toniatti C, Rowley M. J Med Chem.
2009 Nov 26;52(22):7170-85.


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