Tasisulam
WebTasisulam (LY573636) is a SPLAM (SPLicing inhibitor sulfonAMide) that bridges RNA binding motif protein 39 (RBM39; CAPERα, HCC1) and DCAF15 for interaction, thereby promoting (CUL4-DDB1-DDA1-DCAF15) E3 ubiquitin ligase complex-mediated RBM39 ubiquitination and subsequent proteasomal degradation. WebNov 8, 2024 · Tasisulam is highly bound to albumin (> 99.7%) and has a long terminal half-life (11 days) that approximates the half-life of circulating albumin . In vitro studies showed tasisulam competitively inhibits CYP2C9, and could therefore affect the clearance and metabolism of sensitive CYP2C9 substrates, such as warfarin and tolbutamide .
Tasisulam
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WebNov 8, 2011 · Abstract. LY573636-sodium (tasisulam) is a small molecule antitumor agent with a novel mechanism of action currently being investigated in a variety of human … WebTasisulam. Tasisulam, a TGF-β/TGF-β type I receptor kinase (ALK5) inhibitor, has been tested in two phase I clinical trials in patients with refractory or malignant solid tumors, including ovarian cancer, to determine the recommended dose for phase II trials [269,270]. From: Biochimica et Biophysica Acta (BBA) - Reviews on Cancer, 2024.
WebINDIANAPOLIS, Dec. 13, 2010 /PRNewswire/ -- Eli Lilly and Company announced today that it has suspended its global Phase III study evaluating tasisulam, an investigational, small-molecule anti-cancer compound, as a second-line treatment for those with unresectable or metastatic melanoma.. Lilly, in consultation with an independent data …
WebTasisulam C11H6BrCl2NO3S2 CID 10160238 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities ... WebJan 14, 2024 · Tasisulam - Eli Lilly Alternative Names: LY 57636; LY573636; LY573636-sodium; Tasisulam sodium Latest Information Update: 14 Jan 2024. Price : $50 * Buy Profile. Adis is an information provider. We do not sell or distribute actual drugs. Final gross price and currency may vary according to local VAT and billing address. ...
WebMay 13, 2024 · Recently, additional molecules have been discovered to act as glue degraders, including the arylsulfonamide drugs indisulam and tasisulam [] that degrade the splicing factors RBM39 (RNA-binding protein 39) and RBM23 by inducing recruitment to CRL4 DCAF15.
WebTasisulam is a anticancer agent and induces apoptosis via the intrinsic pathway, resulting in cytochrome c release and caspase-dependent cell death. Tasisulam inhibits mitotic … roads and bridges contractors choice awardsWebAug 20, 2010 · The AUCalb is a surrogate marker for unbound tasisulam, and this dosing approach represents the maximum level of unbound tasisulam which may be achieved clinically, administered on Day 1. Period 3: Individualized tasisulam dose (based on AUCalb) administered on Day 1 and 500 mg tolbutamide administered on Day 4. snatcher plushWebNot surprisingly, CQS and tasisulam were also toxic to HCT-116 cells (IC 50 = 7.1 and 6.5 μM, respectively), and a cell line carrying the RBM39 G268V mutation was insensitive to … roads and bridges apWebDec 14, 2010 · Tasisulam, an investigational, small-molecule anti-cancer compound, is part of an extensive clinical development program across a wide range of tumors, including soft tissue sarcoma, breast ... roads and buildings telanganaWebNov 1, 2009 · Have previously completed or withdrawn from this study or any other study investigating tasisulam-sodium. Have a known hypersensitivity to paclitaxel or Cremophor EL (polyoxyethylated castor oil). Are pregnant or lactating. Have received a recent (within 30 days before enrollment) or are receiving concurrent yellow fever vaccination. snatcher plushieWebTasisulam. (Synonyms: LY 573636) Tasisulam is a anticancer agent and induces apoptosis via the intrinsic pathway, resulting in cytochrome c release and caspase … snatcher pointsWebOct 3, 2006 · Tasisulam dose is dependent on participant's height, weight, and gender and is adjusted to target a specific Cmax based on participant laboratory parameters. … roads and earthworks foreman