7-O-(Amino-PEG4)-paclitaxel is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
7-O-(Cbz-N-amido-PEG4)-paclitaxel is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
Paclitaxel-SMCC is a paclitaxel derivative with a SMCC linker. (Succinimidyl-4-( N -maleimidomethyl)cyclohexane-1-carboxylate). Paclitaxel-SMCC can be used to synthesize Paclitaxel bioconjugates with enzymes, antobodies, antigens and other biopolymers. Pa
Paclitaxel-MVCP ( MC-val-cit-pab-paclitaxel )is a paclitaxel derivative with an MC-Val-Cit-PAB linker, which can be used for the preparation of Paclitaxel conjugates for drug delivery and nanomedicine research.
Paclitaxel-Succinic acid (paclitaxel-succinate , paclitaxel-semisucinic acid)is a paclitaxel derivative with a succinic acid linker. Paclitaxel-Succinic acid can be used to prepare paclitaxel conjugates for drug delivery and nanomedicine research.
Paclitaxel octadecanedioate is a prodrug form of paclitaxel that is comprised of paclitaxel conjugated to 1,18-octadecanedioic acid.1 Unlike paclitaxel, it does not promote tubulin polymerization in vitro when used at a concentration of 10 μM. A 5:1 mixture of paclitaxel octadecanedioate:human serum albumin (HSA) is cytotoxic to HT-1080, PANC-1, and HT-29 cells (IC50s = 12, 2.48, and 8.62 nM, respectively). This mixture reduces tumor growth and increases survival in an HT-1080 mouse xenograft model in a dose-dependent manner. |1. Callmann, C.E., Leguyader, C.L.M., Burton, S.T., et al. Antitumor activity of 1,18-octadecanedioic acid-paclitaxel complexed with human serum albumin. J. Am. Chem. Soc. 141(30), 11765-11769 (2019).
DHA-paclitaxel, also know as Taxoprexin, is prodrug comprised of the naturally occurring omega-3 fatty acid docosahexaenoic acid (DHA) covalently conjugated to the anti-microtubule agent paclitaxel. Because tumor cells take up DHA, DHA-paclitaxel is delivered directly to tumor tissue, where the paclitaxel moiety binds to tubulin and inhibits the disassembly of microtubules, thereby resulting in the inhibition of cell division. Paclitaxel also induces apoptosis by binding to and blocking the function of the apoptosis inhibitor protein Bcl-2 (B-cell Leukemia 2). DHA-paclitaxel exhibits improved pharmacokinetic and toxicity profiles when compared to conventional paclitaxel and has demonstrated antineoplastic activity in animal models of cancer.
LY3325656 is a GPR142 agonist suitable for clinical testing in human. LY3325656 demonstrated anti-diabetic benefits in pre-clinical studies and ADME PK properties suitable for human dosing. LY3325656 is the first GPR142 agonist molecule advancing to phase 1 clinic trials for the treatment of Type 2 diabetes.