Chemical Property of Talabostat mesylate
Chemical Property:
- PSA：149.54000
- LogP:0.61560
- Storage Temp.:under inert gas (nitrogen or Argon) at 2–8 °C
- Solubility.:Soluble in DMSO (up to at least 25 mg/ml)
- Hydrogen Bond Donor Count:4
- Hydrogen Bond Acceptor Count:7
- Rotatable Bond Count:3
- Exact Mass:310.1369878
- Heavy Atom Count:20
- Complexity:328
- Purity/Quality:
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99% *data from raw suppliers
Talabostat Mesylate *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:B(C1CCCN1C(=O)C(C(C)C)N)(O)O.CS(=O)(=O)O
- Isomeric SMILES:B([C@@H]1CCCN1C(=O)[C@H](C(C)C)N)(O)O.CS(=O)(=O)O
- Recent ClinicalTrials:Talabostat and Pembrolizumab for the Treatment of Advanced Solid Cancers
- Recent EU Clinical Trials:A Phase 1b/2 Study of BXCL701, a Small Molecule Inhibitor of Dipeptidyl Peptidases (DPP), Administered in Combination with the Anti-Programmed Cell Death 1 (PD-1) Monoclonal Antibody Pembrolizumab (PEMBRO; Keytruda?) in Patients with mCRPC either Small Cell Neuroendocrine Prostate Cancer (SCNC; NEPC) or Adenocarcinoma Phenotype
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Description
Talabostat is a non-selective inhibitor of dipeptidyl peptidases (DPPs), including DPP-4, DPP-7, DPP-8, DPP-9, fibroblast activation protein (FAP), and prolyl endopeptidase (PREP; IC50s = >4, 310, 4, 11, 560, and 390 nM, respectively). It inhibits proliferation of superantigen-stimulated human peripheral blood mononuclear cells (PBMCs; IC50 = ~10 nM). Talabostat (5 μg twice per day) increases expression of a variety of cytokines, including those encoding IL-1β, IL-6, and G-CSF, and chemokines in tumors and tumor-draining lymph nodes in a WEHI-164 fibrosarcoma mouse model. It reduces tumor growth in WEHI-164, MM45T.Sp, and MM52.T fibrosarcoma, EL-4 and A20/2J lymphoma, B16/F10 melanoma, and P815 mastocytoma syngeneic mouse models. Talabostat also increases the efficacy of the antitumor antibodies rituximab and trastuzumab in Namalwa B cell lymphoma and LS180 colon carcinoma mouse xenograft models, respectively.
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Uses
Treatment of cancer; hematopoetic stimulant. Talabostat Mesylate can be used in biological study and pharmacological activity of treatment of cancer using immunomodulation.
