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

OT-82 

Cat. No.: HY-136241
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 Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

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].

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.
Molecular Weight

424.47

Formula

C₂₆H₂₁FN₄O

CAS No.

1800487-55-1

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

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product name:
OT-82
Cat. No.:
HY-136241
Quantity:
MCE Japan Authorized Agent: