B-Raf inhibitor - CAS 1315330-11-0
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Not Intended for Therapeutic Use. For research use only.
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aA B-Raf inhibitor, pyrazine and pyrrolo[2,3-b]pyridine derivatives, useful in the treatment of cancer and proliferative diseases.
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Benzamide, N-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-4-methyl-3-[(6-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy]-
1.Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling.
Liu L1, Lee MR2, Kim JL3, Whittington DA3, Bregman H4, Hua Z4, Lewis RT4, Martin MW4, Nishimura N5, Potashman M4, Yang K5, Yi S4, Vaida KR4, Epstein LF3, Babij C6, Fernando M6, Carnahan J6, Norman MH5. Bioorg Med Chem. 2016 May 15;24(10):2215-34. doi: 10.1016/j.bmc.2016.03.055. Epub 2016 Apr 13.
One of the challenges for targeting B-Raf(V600E) with small molecule inhibitors had been achieving adequate selectivity over the wild-type protein B-Raf(WT), as inhibition of the latter has been associated with hyperplasia in normal tissues. Recent studies suggest that B-Raf inhibitors inducing the 'DFG-in/αC-helix-out' conformation (Type IIB) likely will exhibit improved selectivity for B-Raf(V600E). To explore this hypothesis, we transformed Type IIA inhibitor (1) into a series of Type IIB inhibitors (sulfonamides and sulfamides 4-6) and examined the SAR. Three selectivity indices were introduced to facilitate the analyses: the B-Raf(V600E)/B-Raf(WT) biochemical ((b)S), cellular ((c)S) selectivity, and the phospho-ERK activation ((p)A). Our data indicates that α-branched sulfonamides and sulfamides show higher selectivities than the linear derivatives. We rationalized this finding based on analysis of structural information from the literature and provided evidence for a monomeric B-Raf-inhibitor complex previously hypothesized to be responsible for the desired B-Raf(V600E) selectivity.
2.Discovery of EBI-907: A highly potent and orally active B-Raf(V600E) inhibitor for the treatment of melanoma and associated cancers.
Lu B1, Cao H1, Cao J2, Huang S1, Hu Q1, Liu D2, Shen R2, Shen X1, Tao W1, Wan H1, Wang D1, Yan Y2, Yang L2, Zhang J2, Zhang L1, Zhang L3, Zhang M2. Bioorg Med Chem Lett. 2016 Feb 1;26(3):819-23. doi: 10.1016/j.bmcl.2015.12.086. Epub 2015 Dec 24.
A novel series of pyrazolo[3,4-c]isoquinoline derivatives was discovered as B-Raf(V600E) inhibitors through scaffold hopping based on a literature lead PLX4720. Further SAR exploration and optimization led to the discovery of potent B-Raf(V600E) inhibitors with good oral bioavailability in rats and dogs. One of the compounds EBI-907 (13g) demonstrated excellent in vivo efficacy in B-Raf(V600E) dependent Colo-205 tumor xenograft models in mouse and is under preclinical studies for the treatment of melanoma and B-Raf(V600E) associated cancers.
3.Preclinical Evaluation of a Novel Orally Available SRC/Raf/VEGFR2 Inhibitor, SKLB646, in the Treatment of Triple-Negative Breast Cancer.
Zheng MW1, Zhang CH1, Chen K1, Huang M2, Li YP1, Lin WT1, Zhang RJ1, Zhong L1, Xiang R3, Li LL2, Liu XY1, Wei YQ1, Yang SY4. Mol Cancer Ther. 2016 Mar;15(3):366-78. doi: 10.1158/1535-7163.MCT-15-0501. Epub 2015 Dec 31.
Triple-negative breast cancer (TNBC) is the most aggressive and deadly breast cancer subtype. To date, chemotherapy is the only systemic therapy and prognosis remains poor. Herein, we report the preclinical evaluation of SKLB646 in the treatment of TNBC; SKLB646 is a novel multiple kinase inhibitor developed by us recently. This compound potently inhibited SRC and VEGFR2 with IC50 values of 0.002 μmol/L and 0.012 μmol/L, respectively. It also considerably inhibited B-Raf and C-Raf with IC50 values of 0.022 and 0.019 μmol/L, respectively. It exhibited significant antiproliferation and antiviability activities against TNBC cell lines. Studies of mechanism of action indicated that SKLB646 inhibited the activation of SRC signaling and blocked the MAPK signaling through inhibiting the Raf kinases. Interestingly, SKLB646 dose dependently downregulated the expression of Fra1, a transcriptional factor that plays a critical role in the epithelial-to-mesenchymal transition.
4.Acquired BRAF inhibitor resistance: A multicenter meta-analysis of the spectrum and frequencies, clinical behaviour, and phenotypic associations of resistance mechanisms.
Johnson DB1, Menzies AM2, Zimmer L3, Eroglu Z4, Ye F5, Zhao S5, Rizos H6, Sucker A3, Scolyer RA7, Gutzmer R8, Gogas H9, Kefford RF10, Thompson JF7, Becker JC11, Berking C12, Egberts F13, Loquai C14, Goldinger SM15, Pupo GM16, Hugo W17, Kong X17, Garraway Eur J Cancer. 2015 Dec;51(18):2792-9. doi: 10.1016/j.ejca.2015.08.022. Epub 2015 Nov 19.
BACKGROUND: Acquired resistance to BRAF inhibitors (BRAFi) is a near-universal phenomenon caused by numerous genetic and non-genetic alterations. In this study, we evaluated the spectrum, onset, pattern of progression, and subsequent clinical outcomes associated with specific mechanisms of resistance.
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