OT-82

Catalog No.S9706 Batch:S970601

Technical Data

Formula	C₂₆H₂₁FN₄O
Molecular Weight	424.47	CAS No.	1800487-55-1
Solubility (25°C)*	In vitro	DMSO	85 mg/mL (200.24 mM)
		Ethanol	85 mg/mL (200.24 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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.<a class="sref" href="#s_ref">[1]</a>

In vivo

OT-82 has therapeutic effect in subcutaneous(SC) and systemic mouse xenograft models of HP malignancies.<a class="sref" href="#s_ref">[1]</a>

Protocol (from reference)

Cell Assay:^{<sup><a class="sref" href="#s_ref">[1]</a></sup>}	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.
Animal Study:^{<sup><a class="sref" href="#s_ref">[1]</a></sup>}	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.

Cell Assay:^{<a class="sref" href="#s_ref">[1]</a>}

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.

Animal Study:^{<a class="sref" href="#s_ref">[1]</a>}

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.

References

[1] Lioubov Korotchkina, et al.Leukemia. 2020 Jul;34(7):1828-1839.

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

Inhibition of nicotinamide dinucleotide salvage pathway counters acquired and intrinsic poly(ADP-ribose) polymerase inhibitor resistance in high-grade serous ovarian cancer [ Sci Rep, 2023, 13(1):3334]	PubMed: 36849518

Inhibition of nicotinamide dinucleotide salvage pathway counters acquired and intrinsic poly(ADP-ribose) polymerase inhibitor resistance in high-grade serous ovarian cancer [ Sci Rep, 2023, 13(1):3334]

PubMed: 36849518

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SHIPPING AND STORAGE
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