Birinapant - CAS 1260251-31-7
Catalog number: B0084-462223
Category: Inhibitor
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Birinapant, also known as TL32711, is a synthetic small molecule and peptido mimetic of second mitochondrial-derived activator of caspases (SMAC) and inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins, with potential antineoplastic activity. As a SMAC mimetic and IAP antagonist, TL32711 binds to and inhibits the activity of IAPs, such as X chromosome-linked IAP (XIAP) and cellular IAPs 1 and 2. Since IAPs shield cancer cells from the apoptosis process, this agent may restore and promote the induction of apoptosis through apoptotic signaling pathways in cancer cells. IAPs are overexpressed by many cancer cell types and suppress apoptosis by binding and inhibiting active caspases-3, -7 and -9 via their baculoviral lAP repeat (BIR) domains. Check for active clinical trials or closed clinical trials using this agent.
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B0084-462223 100 mg $798 In stock
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white solid powder
TL-32711; TL32711; TL 32711. Birinapant
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TetraLogic Pharmaceuticals.
1.Discovery of Novel, Potent, and Specific Cell-Death Inducers in the Jurkat Acute Lymphoblastic Leukemia Cell Line.
Carosati E1, van den Höfel N2, Reif M2, Randazzo GM3, Stanitzki B2, Stevens J2, Gabbert HE2, Cruciani G3, Mannhold R4, Mahotka C5. ChemMedChem. 2015 Oct;10(10):1700-6. doi: 10.1002/cmdc.201500245. Epub 2015 Aug 12.
The limited clinical efficacy of many cancer therapeutics has initiated intense research efforts toward the discovery of novel chemical entities in this field. In this study, 31 hit candidates were selected from nearly 800,000 database compounds in a ligand-based virtual screening campaign. In turn, three of these hits were found to have (sub)micromolar potencies in proliferation assays with the Jurkat acute lymphatic leukemic cell line. In this assay, the three hits were found to exhibit higher potency than clinically tested cell-death inducers (GDC-0152, AT-406, and birinapant). Importantly, antiproliferative activity toward non-cancer peripheral blood mononuclear cells (PBMCs) was found to be marginal. Further biological characterization demonstrated the cell-death-inducing properties of these compounds. Biological testing of hit congeners excluded a nonspecific, toxic effect of the novel structures. Altogether, these findings may have profound relevance for the development of clinical candidates in tumor therapy.
2.Targeting p38 or MK2 Enhances the Anti-Leukemic Activity of Smac-Mimetics.
Lalaoui N1, Hänggi K2, Brumatti G1, Chau D1, Nguyen NY3, Vasilikos L2, Spilgies LM2, Heckmann DA1, Ma C1, Ghisi M4, Salmon JM4, Matthews GM4, de Valle E5, Moujalled DM3, Menon MB6, Spall SK1, Glaser SP1, Richmond J7, Lock RB7, Condon SM8, Gugasyan R5, Gae Cancer Cell. 2016 Feb 8;29(2):145-58. doi: 10.1016/j.ccell.2016.01.006.
Birinapant is a smac-mimetic (SM) in clinical trials for treating cancer. SM antagonize inhibitor of apoptosis (IAP) proteins and simultaneously induce tumor necrosis factor (TNF) secretion to render cancers sensitive to TNF-induced killing. To enhance SM efficacy, we screened kinase inhibitors for their ability to increase TNF production of SM-treated cells. We showed that p38 inhibitors increased TNF induced by SM. Unexpectedly, even though p38 is required for Toll-like receptors to induce TNF, loss of p38 or its downstream kinase MK2 increased induction of TNF by SM. Hence, we show that the p38/MK2 axis can inhibit or promote TNF production, depending on the stimulus. Importantly, clinical p38 inhibitors overcame resistance of primary acute myeloid leukemia to birinapant.
3.Promises and Challenges of Smac Mimetics as Cancer Therapeutics.
Fulda S1. Clin Cancer Res. 2015 Nov 15;21(22):5030-6. doi: 10.1158/1078-0432.CCR-15-0365.
Inhibitor of Apoptosis (IAP) proteins block programmed cell death and are expressed at high levels in various human cancers, thus making them attractive targets for cancer drug development. Second mitochondrial activator of caspases (Smac) mimetics are small-molecule inhibitors that mimic Smac, an endogenous antagonist of IAP proteins. Preclinical studies have shown that Smac mimetics can directly trigger cancer cell death or, even more importantly, sensitize tumor cells for various cytotoxic therapies, including conventional chemotherapy, radiotherapy, or novel agents. Currently, several Smac mimetics are under evaluation in early clinical trials as monotherapy or in rational combinations (i.e., GDC-0917/CUDC-427, LCL161, AT-406/Debio1143, HGS1029, and TL32711/birinapant). This review discusses the promise as well as some challenges at the translational interface of exploiting Smac mimetics as cancer therapeutics.
4.Effect of a Smac Mimetic (TL32711, Birinapant) on the Apoptotic Program and Apoptosis Biomarkers Examined with Validated Multiplex Immunoassays Fit for Clinical Use.
Srivastava AK1, Jaganathan S2, Stephen L3, Hollingshead MG4, Layhee A3, Damour E3, Govindharajulu JP2, Donohue J3, Esposito D5, Mapes JP3, Kinders RJ2, Takebe N6, Tomaszewski JE7, Kummar S7, Doroshow JH7, Parchment RE2. Clin Cancer Res. 2016 Feb 15;22(4):1000-10. doi: 10.1158/1078-0432.CCR-14-3156. Epub 2015 Oct 7.
PURPOSE: To support clinical pharmacodynamic evaluation of the Smac mimetic TL32711 (birinapant) and other apoptosis-targeting drugs, we describe the development, validation, and application of novel immunoassays for 15 cytosolic and membrane-associated proteins indicative of the induction, onset, and commitment to apoptosis in human tumors.
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