B-Raf IN 1 - CAS 950736-05-7
Catalog number:
950736-05-7
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C29H24F3N5O
Molecular Weight:
515.53
COA:
Inquire
Targets:
Raf
Description:
B-Raf IN 1 is a highlt potent and selective B-Raf inhibitor. It was equipotent against c-Raf.
Publictions citing BOC Sciences Products
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Purity:
>98%
MSDS:
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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.Phospho-proteomic analyses of B-Raf protein complexes reveal new regulatory principles.
Eisenhardt AE1,2,3, Sprenger A3,4,5, Röring M1,2,3,6, Herr R1,2,3, Weinberg F1,2,3, Köhler M1,2,3,6, Braun S1,2,3, Orth J4, Diedrich B3,7, Lanner U3, Tscherwinski N2,3, Schuster S2,3, Dumaz N5, Schmidt E2,3, Baumeister R2,3,8,9, Schlosser A2,3,10, Dengjel Oncotarget. 2016 Mar 28. doi: 10.18632/oncotarget.8427. [Epub ahead of print]
B-Raf represents a critical physiological regulator of the Ras/RAF/MEK/ERK-pathway and a pharmacological target of growing clinical relevance, in particular in oncology. To understand how B-Raf itself is regulated, we combined mass spectrometry with genetic approaches to map its interactome in MCF-10A cells as well as in B-Raf deficient murine embryonic fibroblasts (MEFs) and B-Raf/Raf-1 double deficient DT40 lymphoma cells complemented with wildtype or mutant B-Raf expression vectors. Using a multi-protease digestion approach, we identified a novel ubiquitination site and provide a detailed B-Raf phospho-map. Importantly, we identify two evolutionary conserved phosphorylation clusters around T401 and S419 in the B-Raf hinge region. SILAC labelling and genetic/biochemical follow-up revealed that these clusters are phosphorylated in the contexts of oncogenic Ras, sorafenib induced Raf dimerization and in the background of the V600E mutation.
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CAS 950736-05-7 B-Raf IN 1

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