Talabostat (mesylate) – 50 mg

Brand:
Cayman
CAS:
150080-09-4
Storage:
-20
UN-No:
Non-Hazardous - /

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).{47719} 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.{47720} 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.  

 

Available on backorder

SKU: 29007 - 50 mg Category:

Description

A non-selective inhibitor of DPPs (IC50s = >4, 310, 4, 11, 560, and 390 nM for DPP-4, DPP-7, DPP-8, DPP-9, FAP, and PREP, respectively); inhibits proliferation of superantigen-stimulated human PBMCs (IC50 = ~10 nM); increases expression of a variety of cytokines and chemokines in tumors and tumor-draining lymph nodes in a WEHI-164 fibrosarcoma mouse model at 5 μg twice per day; reduces tumor growth in a variety of syngeneic mouse models; increases the efficacy of the antitumor antibodies rituximab and trastuzumab in Namalwa B cell lymphoma and LS180 colon carcinoma mouse xenograft models, respectively


Formal name: B-[(2R)-1-[(2S)-2-amino-3-methyl-1-oxobutyl]-2-pyrrolidinyl]-boronic acid, methanesulfonate

Synonyms:  Val-boro-Pro

Molecular weight: 310.2

CAS: 150080-09-4

Purity: ≥95%

Formulation: A solid