Home Metabolism NAMPT inhibitor OT-82 For research use only.

OT-82

OT-82 is a novel nicotinamide phosphoribosyltransferase (NAMPT) inhibitor with average IC50s of 13.03   nM in non-HP cancer cells and 2.89   nM in HP cancer cells, respectively.

OT-82 Chemical Structure

OT-82 Chemical Structure

CAS: 1800487-55-1

Selleck's OT-82 has been cited by 1 publication

Purity & Quality Control

Batch: S970601 DMSO] 85 mg/mL] false] Ethanol] 85 mg/mL] false] Water] Insoluble] false Purity: 99.96%
99.96

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Biological Activity

Description OT-82 is a novel nicotinamide phosphoribosyltransferase (NAMPT) inhibitor with average IC50s of 13.03   nM in non-HP cancer cells and 2.89   nM in HP cancer cells, respectively.
Targets
NAMPT [1]
(in hematopoietic cells)
2.89 nM
In vitro
In vitro

OT-82 is an effective nicotinamide phosphoribosyltransferase (NAMPT) inhibitor, thus inhibits the salvage pathway of NAD synthesis to kill the neoplastic cells of hematopoietic. The average IC50 is 13.03 nM in non-HP cancer cells and 2.89 nM in HP cancer cells.<sup><a class="sref" href="#s_ref">[1]</a></sup>
Cell Research Cell lines MV4–11 cells
Concentrations --
Incubation Time 1 h
Method

MV4 11 cell extract (3 mg protein/reaction) was incubated for 1 h at 40 ℃ with Affi-Gel 10 coupled with "active" compound (OT-82), "inactive" compound (a non-cytotoxic OT- 82 structural analog), or a combination of the two ("competition"). Eluted proteins were subjected to gel electrophoresis and silver staining or transferred to nitrocellulose membrane for western blotting with NAMPT antisera.
In Vivo
In vivo

OT-82 has therapeutic effect in subcutaneous(SC) and systemic mouse xenograft models of HP malignancies.<sup><a class="sref" href="#s_ref">[1]</a></sup>
Animal Research Animal Models Ubcutaneous (SC) and systemic mouse xenograft models of HP malignancies
Dosages 25 or 50 mg/kg for 6 consecutive days per week for 3 weeks
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03921879 Unknown status
Lymphoma|Lymphoma Non-Hodgkin|Lymphoma B-Cell|Lymphoma T-Cell|Lymphoma Follicular|Lymphoma Peripheral T-Cell|Lymphoma Hodgkin
Oncotartis Inc.
 July 29 2019 Phase 1

Chemical Information & Solubility

Molecular Weight 424.47 Formula

C26H21FN4O
CAS No. 1800487-55-1 SDF --
Smiles FC1=CC=C(C=C1)C#CC2=CC(=CC=C2C3=CC=NC=C3)C(=O)NCCCC4=C[NH]N=C4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 85 mg/mL ( (200.24 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 85 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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