WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 207115
CAS#: 1800487-55-1 (free base)
Description: OT-82 is a potent NAMPT Inhibitor that targets the strong dependence of hematological malignancies on NAD biosynthesis. OT-82 showed strong efficacy against hematopoietic malignancies including acute myeloblastic and lymphoblastic adult and pediatric leukemias, erythroleukemia, multiple myeloma, and Burkitt's lymphoma in vitro and in mouse xenograft models.
MedKoo Cat#: 207115
CAS#: 1800487-55-1 (free base)
Chemical Formula: C26H21FN4O
Exact Mass: 424.1699
Molecular Weight: 424.4794
Elemental Analysis: C, 73.57; H, 4.99; F, 4.48; N, 13.20; O, 3.77
Synonym: OT-82; OT 82; OT82; NAMPTi OT-82; nicotinamide phosphoribosyl transferase inhibitor OT-82;
IUPAC/Chemical Name: N-(3-(1H-pyrazol-4-yl)propyl)-3-((4-fluorophenyl)ethynyl)-4-(pyridin-4-yl)benzamide
InChi Key: CEPAXRIKSUXHHB-UHFFFAOYSA-N
InChi Code: InChI=1S/C26H21FN4O/c27-24-8-4-19(5-9-24)3-6-22-16-23(7-10-25(22)21-11-14-28-15-12-21)26(32)29-13-1-2-20-17-30-31-18-20/h4-5,7-12,14-18H,1-2,13H2,(H,29,32)(H,30,31)
SMILES Code: O=C(C1=CC(C#CC2=CC=C(C=C2)F)=C(C=C1)C3=CC=NC=C3)NCCCC4=CNN=C4
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 424.4794 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Korotchkina L, Kazyulkin D, Komarov PG, Polinsky A, Andrianova EL, Joshi S,
Gupta M, Vujcic S, Kononov E, Toshkov I, Tian Y, Krasnov P, Chernov MV, Veith J,
Antoch MP, Middlemiss S, Somers K, Lock RB, Norris MD, Henderson MJ, Haber M,
Chernova OB, Gudkov AV. OT-82, a novel anticancer drug candidate that targets the
strong dependence of hematological malignancies on NAD biosynthesis. Leukemia.
2020 Jan 2. doi: 10.1038/s41375-019-0692-5. [Epub ahead of print] PubMed PMID:
2: Somers K, Evans K, Cheung L, Karsa M, Pritchard T, Kosciolek A, Bongers A,
El-Ayoubi A, Forgham H, Middlemiss S, Mayoh C, Jones L, Gupta M, Kees UR,
Chernova O, Korotchkina L, Gudkov AV, Erickson SW, Teicher B, Smith MA, Norris
MD, Haber M, Lock RB, Henderson MJ. Effective targeting of NAMPT in
patient-derived xenograft models of high-risk pediatric acute lymphoblastic
leukemia. Leukemia. 2019 Dec 17. doi: 10.1038/s41375-019-0683-6. [Epub ahead of
print] PubMed PMID: 31848452.
OT-82 binds to and inhibits the activity of NAMPT. This depletes cellular NAD and inhibits NAD-dependent enzymes, both of which are needed for rapid cell proliferation; this results in cell death in NAMPT-overexpressing cancer cells. NAMPT, an enzyme that is responsible for maintaining the intracellular NAD pool, plays a key role in the regulation of cellular metabolism and has cytokine-like activities. NAMPT is overexpressed in a variety of cancers and metabolic disorders; tumor cells rely on NAMPT activity for their NAD supply