RAF265 - CAS 927880-90-8
Catalog number: B0084-286688
Category: Inhibitor
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RAF265 is a potent selective inhibitor of C-Raf/B-Raf/B-Raf V600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM.
CHIR-265; RAF265; CHIR 265; RAF 265; CHIR265; RAF-265
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1.Synergistic antitumour activity of RAF265 and ZSTK474 on human TT medullary thyroid cancer cells.
Bertazza L1, Barollo S1, Radu CM2, Cavedon E1, Simioni P2, Faggian D3, Plebani M3, Pelizzo MR4, Rubin B1, Boscaro M1, Pezzani R1, Mian C1. J Cell Mol Med. 2015 Sep;19(9):2244-52. doi: 10.1111/jcmm.12612. Epub 2015 Jun 17.
Medullary thyroid cancer (MTC) is an aggressive malignancy responsible for up to 14% of all thyroid cancer-related deaths. It is characterized by point mutations in the rearranged during transfection (RET) proto-oncogene. The activated RET kinase is known to signal via extracellular signal regulated kinase (ERK) and phosphoinositide 3-kinase (PI3K), leading to enhanced proliferation and resistance to apoptosis. In the present work, we have investigated the effect of two serine/threonine-protein kinase B-Raf (BRAF) inhibitors (RAF265 and SB590885), and a PI3K inhibitor (ZSTK474), on RET-mediated signalling and proliferation in a MTC cell line (TT cells) harbouring the RETC634W activating mutation. The effects of the inhibitors on VEGFR2, PI3K/Akt and mitogen-activated protein kinases signalling pathways, cell cycle, apoptosis and calcitonin production were also investigated. Only the RAF265+ ZSTK474 combination synergistically reduced the viability of treated cells.
2.Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.
Williams TE1, Subramanian S1, Verhagen J1, McBride CM1, Costales A1, Sung L1, Antonios-McCrea W1, McKenna M1, Louie AK1, Ramurthy S1, Levine B1, Shafer CM1, Machajewski T1, Renhowe PA1, Appleton BA1, Amiri P1, Chou J1, Stuart D1, Aardalen K1, Poon D1. ACS Med Chem Lett. 2015 Aug 3;6(9):961-5. doi: 10.1021/ml500526p. eCollection 2015.
Abrogation of errant signaling along the MAPK pathway through the inhibition of B-RAF kinase is a validated approach for the treatment of pathway-dependent cancers. We report the development of imidazo-benzimidazoles as potent B-RAF inhibitors. Robust in vivo efficacy coupled with correlating pharmacokinetic/pharmacodynamic (PKPD) and PD-efficacy relationships led to the identification of RAF265, 1, which has advanced into clinical trials.
3.The combination of RAF265, SB590885, ZSTK474 on thyroid cancer cell lines deeply impact on proliferation and MAPK and PI3K/Akt signaling pathways.
Barollo S1, Bertazza L, Baldini E, Ulisse S, Cavedon E, Boscaro M, Pezzani R, Mian C. Invest New Drugs. 2014 Aug;32(4):626-35. doi: 10.1007/s10637-014-0108-3. Epub 2014 May 13.
Papillary thyroid cancer (PTC) is the most frequent thyroid cancer entity, accounting for 88 % of cases. It may metastasize and loose iodine uptake capability, preventing any radioiodine or surgical treatment. The main gene altered in PTC is BRAF, which is found altered in over 50 % of cases. Moreover MAPK and PI3K/Akt pathways are greatly implicated in PTC development. Many target therapies for PTC are currently under investigation, unfortunately without the expected results. Aim of this study was to characterized the preclinical effectiveness of novel promising drugs, RAF265, SB590885 and ZSTK474 in 3 thyroid cancer cell lines (BCPAP, K1, 8505C). RAF265 and SB590885 target differentially BRAF, while ZSTK474 acts on PI3K. IC50 demonstrated high drug activities ranging from 0.1 to 6.2 μM, depending on drugs and cell type, while combination index revealed an interesting synergistic effect of combination regimen (RAF265 + ZSTK474 and SB590885 + ZSTK474) in almost all cell lines.
4.Preclinical analysis of the anti-tumor and anti-metastatic effects of Raf265 on colon cancer cells and CD26(+) cancer stem cells in colorectal carcinoma.
Chow AK1, Cheng NS2, Lam CS3, Ng L4, Wong SK5, Wan TM6, Man JH7, Cheung AH8, Yau TC9, Poon JT10, Law WL11, Pang RW12. Mol Cancer. 2015 Apr 11;14:80. doi: 10.1186/s12943-015-0352-y.
BACKGROUND: In colorectal carcinoma (CRC), activation of the Raf/MEK/ERK signaling pathway is commonly observed. In addition, the commonly used 5FU-based chemotherapy in patients with metastatic CRC was found to enrich a subpopulation of CD26(+) cancer stem cells (CSCs). As activation of the Raf/MEK/ERK signaling pathway was also found in the CD26(+) CSCs and therefore, we hypothesized that an ATP-competitive pan-Raf inhibitor, Raf265, is effective in eliminating the cancer cells and the CD26(+) CSCs in CRC patients.
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CAS 927880-90-8 RAF265

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