1. Metabolic Enzyme/Protease
  2. NAMPT
  3. OT-82

OT-82 

Cat. No.: HY-136241 Purity: 99.84%
Handling Instructions

OT-82 is a potent, selective and orally active inhibitor of NAMPT. OT-82 is selectively toxic to cells of hematopoietic origin and induces cell death in a NAD+ dependent manner. OT-82 is a promising antineoplastic agent for the study of hematological malignancies.

For research use only. We do not sell to patients.

OT-82 Chemical Structure

OT-82 Chemical Structure

CAS No. : 1800487-55-1

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 440 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 440 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 400 In-stock
Estimated Time of Arrival: December 31
10 mg USD 680 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1950 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2900 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

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Description

OT-82 is a potent, selective and orally active inhibitor of NAMPT. OT-82 is selectively toxic to cells of hematopoietic origin and induces cell death in a NAD+ dependent manner. OT-82 is a promising antineoplastic agent for the study of hematological malignancies[1].

IC50 & Target

IC50: Nampt[1]

In Vitro

OT-82 (0.0001-10 μM; 72 hours) demonstrates tissue-selective (HP vs non-HP) cytotoxicity. It is against HP cell lines MV4–11, U937, RS4;11, HEL92.1.7 and PER485 cell growth with IC50 values of 2.11 nM, 2.70 nM, 1.05 nM and 1.36 nM, respectively. It also against nonHP cell lines MCF-7, U87, HT29, and H1299 cell growth with IC50 values of 37.92 nM, 29.52 nM, 15.67 nM and 7.95 nM , respectively[1].
OT-82 demonstrates cancer-selective (tumor vs normal) cytotoxicity. It more sensitive to BMMNC from leukemia patients, the IC50 values are 31 nM and 7.10 nM for AML and ALL donors, respectively. The IC50 value is 62.69 nM for BMMNC from healthy donors[1].
OT-82 (0.001-10 μM; 48 hours) inhibits recombinant NAMPT activity and causes dose-dependent reductions in cellular NAD and ATP concentrations in MV4–11 cells[1].
OT-82 (0.01-100 nM; 48 hours) results in activation of caspase-3, an increase in the proportion of cells with sub-G1 DNA content, and depolarization of the mitochondrial membrane in MV4–11 cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: HP cell lines (MV4–11, U937, RS4;11, HEL92.1.7, PER485)
Non-HP cell lines (MCF-7, U87, HT29, H1299)
Concentration: 0.0001 μM-10 μM
Incubation Time: 72 hours
Result: Was against human cell lines derived from hematological malignancies (HP) with IC50 values ranging from 1.10 nM to 5.86 nM, and was against non-HP cancers with IC50 ranging from 1.10 nM to 37.92 nM[1].

Apoptosis Analysis[1]

Cell Line: MV4–11 cells
Concentration: 0.01-100 nM
Incubation Time: 48 hours
Result: Exhibited hallmarks of apoptotic cell death
In Vivo

OT-82 (oral gavage; 20 or 40 mg/kg; 3 weeks) treatment increases survival to 100% and 56% at 40 or 20 mg/kg, respectively after treatment discontinuation in SC xenograft model of Burkitt's lymphoma[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SC xenograft model of Burkitt's lymphoma in SCID mice[1]
Dosage: 20 or 40 mg/kg
Administration: oral gavage; 3 weeks
Result: Potently inhibited tumor growth of multiple myeloma mouse model.
Clinical Trial
Molecular Weight

424.47

Formula

C₂₆H₂₁FN₄O

CAS No.
SMILES

O=C(NCCCC1=CNN=C1)C2=CC=C(C3=CC=NC=C3)C(C#CC4=CC=C(F)C=C4)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (235.59 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3559 mL 11.7794 mL 23.5588 mL
5 mM 0.4712 mL 2.3559 mL 4.7118 mL
10 mM 0.2356 mL 1.1779 mL 2.3559 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.90 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.90 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.90 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.84%

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Keywords:

OT-82OT82OT 82NAMPTNicotinamide phosphoribosyl transferasePBEFVisfatinpre-B cell-enhancing factorPre-B cell colony enhancing factorNAMPTiHematologicalmalignancYMV4–11THP1PER485CCRF-HSB2ErythroleukemiaRamosMel-7A549MCF-7BreastcarcinomaHCT116metabolicdisordersLymphoma,?Non-HodgkinInhibitorinhibitorinhibit

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OT-82
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