CPI-203 - CAS 1446144-04-2
Catalog number: B0084-463432
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
BET Bromodomain
CPI-203 is a BET bromodomain inhibitor. It inhibits BRD4 in vitro and in cells, and causes G1 cell cycle arrest. It also arrests the growth of T cell acute lymphoblastic leukemia cells in vitro (EC50 = 91.2 nM).
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-463432 25 mg $299 In stock
B0084-463432 100 mg $499 In stock
B0084-463432 500 mg $1299 In stock
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Brife Description:
BET Bromodomain inhibitor
Store at -20°C
Shelf Life:
2 years
Canonical SMILES:
1.Synergistic antitumor activity of lenalidomide with the BET bromodomain inhibitor CPI203 in bortezomib-resistant mantle cell lymphoma.
Moros A;Rodríguez V;Saborit-Villarroya I;Montraveta A;Balsas P;Sandy P;Martínez A;Wiestner A;Normant E;Campo E;Pérez-Galán P;Colomer D;Roué G Leukemia. 2014 Oct;28(10):2049-59. doi: 10.1038/leu.2014.106. Epub 2014 Mar 18.
Bortezomib therapy has shown promising clinical activity in mantle cell lymphoma (MCL), but the development of resistance to proteasome inhibition may limit its efficacy. To unravel the factors involved in the acquisition of bortezomib resistance in vivo, immunodeficient mice were engrafted with a set of MCL cell lines with different levels of sensitivity to the drug, followed by gene expression profiling of the tumors and functional validation of the identified gene signatures. We observed an increased tumorigenicity of bortezomib-resistant MCL cells in vivo, which was associated with plasmacytic differentiation features, like interferon regulatory factor 4 (IRF4) and Blimp-1 upregulation. Lenalidomide was particularly active in this subgroup of tumors, targeting IRF4 expression and plasmacytic differentiation program, thus overcoming bortezomib resistance. Moreover, repression of the IRF4 target gene MYC in bortezomib-resistant cells by gene knockdown or treatment with CPI203, a BET (bromodomain and extra terminal) bromodomain inhibitor, synergistically induced cell death when combined with lenalidomide. In mice, addition of CPI203 to lenalidomide therapy further decreased tumor burden, involving simultaneous MYC and IRF4 downregulation and apoptosis induction.
2.The BET bromodomain inhibitor CPI203 improves lenalidomide and dexamethasone activity in
Díaz T;Rodríguez V;Lozano E;Mena MP;Calderón M;Rosiñol L;Martínez A;Tovar N;Pérez-Galán P;Bladé J;Roué G;de Larrea CF Haematologica. 2017 Oct;102(10):1776-1784. doi: 10.3324/haematol.2017.164632. Epub 2017 Jul 27.
Most patients with multiple myeloma treated with current therapies, including immunomodulatory drugs, eventually develop relapsed/refractory disease. Clinical activity of lenalidomide relies on degradation of Ikaros and the consequent reduction in IRF4 expression, both required for myeloma cell survival and involved in the regulation of MYC transcription. Thus, we sought to determine the combinational effect of an MYC-interfering therapy with lenalidomide/dexamethasone. We analyzed the potential therapeutic effect of the combination of the BET bromodomain inhibitor CPI203 with the lenalidomide/dexamethasone regimen in myeloma cell lines. CPI203 exerted a dose-dependent cell growth inhibition in cell lines, indeed in lenalidomide/dexamethasone-resistant cells (median response at 0.5 μM: 65.4%), characterized by G1 cell cycle blockade and a concomitant inhibition of MYC and Ikaros signaling. These effects were potentiated by the addition of lenalidomide/dexamethasone. Results were validated in primary plasma cells from patients with multiple myeloma co-cultured with the mesenchymal stromal cell line stromaNKtert. Consistently, the drug combination evoked a 50% reduction in cell proliferation and correlated with basal Ikaros mRNA expression levels (;P;=0.
3.Selective and reversible suppression of intestinal stem cell differentiation by pharmacological inhibition of BET bromodomains.
Nakagawa A;Adams CE;Huang Y;Hamarneh SR;Liu W;Von Alt KN;Mino-Kenudson M;Hodin RA;Lillemoe KD;Fernández-Del Castillo C;Warshaw AL;Liss AS Sci Rep. 2016 Feb 9;6:20390. doi: 10.1038/srep20390.
Absorptive and secretory cells of the small intestine are derived from a single population of Lgr5-expressing stem cells. While key genetic pathways required for differentiation into specific lineages have been defined, epigenetic programs contributing to this process remain poorly characterized. Members of the BET family of chromatin adaptors contain tandem bromodomains that mediate binding to acetylated lysines on target proteins to regulate gene expression. In this study, we demonstrate that mice treated with a small molecule inhibitor of BET bromodomains, CPI203, exhibit greater than 90% decrease in tuft and enteroendocrine cells in both crypts and villi of the small intestine, with no changes observed in goblet or Paneth cells. BET bromodomain inhibition did not alter the abundance of Lgr5-expressing stem cells in crypts, but rather exerted its effects on intermediate progenitors, in part through regulation of Ngn3 expression. When BET bromodomain inhibition was combined with the chemotherapeutic gemcitabine, pervasive apoptosis was observed in intestinal crypts, revealing an important role for BET bromodomain activity in intestinal homeostasis. Pharmacological targeting of BET bromodomains defines a novel pathway required for tuft and enteroendocrine differentiation and provides an important tool to further dissect the progression from stem cell to terminally differentiated secretory cell.
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CAS 1446144-04-2 CPI-203

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