OT-82 |
カタログ番号GC60278
One-Click Copy Product Info
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OT-82 は、NAMPT の強力で選択的な経口活性阻害剤です。 OT-82 は造血系細胞に対して選択的に毒性があり、NAD+ 依存的に細胞死を誘導します。 OT-82 は、血液悪性腫瘍の研究に有望な抗腫瘍薬です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1800487-55-1
Sample solution is provided at 25 µL, 10mM.
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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].
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)
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]
[1]. Korotchkina L, et al. OT-82, a novel anticancer drug candidate that targets the strong dependence of hematological malignancies on NAD biosynthesis.Leukemia. 2020 Jan 2.
| Cas No. | 1800487-55-1 | SDF | |
| Canonical SMILES | O=C(NCCCC1=CNN=C1)C2=CC=C(C3=CC=NC=C3)C(C#CC4=CC=C(F)C=C4)=C2 | ||
| Formula | C26H21FN4O | M.Wt | 424.47 |
| 溶解度 | Storage | Store at -20°C | |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3559 mL | 11.7794 mL | 23.5588 mL |
| 5 mM | 471.2 μL | 2.3559 mL | 4.7118 mL |
| 10 mM | 235.6 μL | 1.1779 mL | 2.3559 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)