| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
The target is NAMPT (Nicotinamide Phosphoribosyltransferase), an enzyme critical for NAD+ biosynthesis. Cancer cells often have a high demand for NAD+, making NAMPT an attractive target for anti-cancer therapy. By inhibiting NAMPT, this compound depletes intracellular NAD+ levels, disrupting energy metabolism and DNA repair pathways, leading to cell death.
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| ln Vitro |
Cellular efficacy against A2780, CORL23, c-Kit, and HER2 expressing cell lines is demonstrated by Nampt-IN-10 TFA (0-1 μM; 72 hours) [1].
Nampt-IN-10 TFA exhibits potent cellular efficacy with low nanomolar IC50 values: 5 nM in A2780 ovarian cancer cells and 19 nM in CORL23 lung cancer cells. This high potency demonstrates its ability to efficiently inhibit NAMPT in living cells and cause cancer cell death. Activity is also demonstrated against c-Kit and HER2-expressing cell lines. |
| ln Vivo |
Specific in vivo data for the unconjugated Nampt-IN-10 TFA are not detailed, as its primary application is as an ADC payload. Its in vivo activity will be determined by the targeting antibody that delivers it to the tumor. As a highly potent cytotoxic agent, it is expected to cause significant tumor regression in xenograft models when conjugated to a tumor-targeting antibody, with reduced systemic toxicity compared to the free drug.
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| Enzyme Assay |
A typical NAMPT biochemical assay measures the formation of the product, nicotinamide mononucleotide (NMN). Purified recombinant NAMPT is incubated with its substrates, nicotinamide and 5-phosphoribosyl-1-pyrophosphate (PRPP), and varying concentrations of Nampt-IN-10 TFA in a reaction buffer. After incubation, the reaction is stopped, and the quantity of NMN produced is measured using a coupled enzyme assay (e.g., using a fluorometric or luminescent NAD+ detection kit).
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| Cell Assay |
Cytotoxicity assay[1]
Cell Types: A2780, CORL23, NCI-H526 expressing c-Kit, MDA-MB453 and NCI-N87 expressing HER2 Cell lines Tested Concentrations: 0-1 μM Incubation Duration: 72 hrs (hours) Experimental Results: Cell potency shown The IC50 values were 5, 19, 2, 0.4, and 1 nM for c-Kit-expressing A2780, CORL23, NCI-H526, HER2-expressing MDA-MB453, and NCI-N87 cells, respectively. The cellular activity is evaluated using A2780 (ovarian) and CORL23 (lung) cancer cells. Cells are seeded in 96-well plates and treated with serial dilutions of Nampt-IN-10 TFA (0-1 microM) for 72 hours. Cell viability is measured using a CellTiter-Glo or an MTS assay to calculate IC50 values. For mechanism studies, cells are treated for 6-24 hours, and intracellular NAD+ levels are measured using a NAD/NADH-Glo assay. Poly (ADP-ribose) polymerase (PARP) cleavage and apoptosis markers are assessed by Western blot. |
| Animal Protocol |
No detailed in vivo protocols are available. A standard study for an ADC payload would evaluate Nampt-IN-10 TFA conjugated to a targeting antibody. For the unconjugated payload, a protocol for maximum tolerated dose (MTD) determination would be performed in mice. The compound would be administered intravenously or intraperitoneally at escalating doses to determine the highest non-lethal dose.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic parameters for Nampt-IN-10 TFA are not detailed in the available literature. However, as a small-molecule payload, its design likely incorporates properties for efficient conjugation and retention within the ADC. When delivered as part of an ADC, the PK of the entire conjugate, not the free payload, is the primary driver of in vivo exposure.
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| Toxicity/Toxicokinetics |
Specific toxicological data for Nampt-IN-10 TFA are not detailed. As a highly potent NAMPT inhibitor, the free drug is expected to have a narrow therapeutic window and significant systemic toxicity due to the essential role of NAD+ in all cells. This is precisely why it is being developed as an ADC payload to target its delivery directly to cancer cells and limit systemic exposure.
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| References | |
| Additional Infomation |
Nampt-IN-10 TFA is an experimental research chemical primarily designed as a novel, non-mitotic ADC payload. It provides an alternative to traditional tubulin inhibitors like MMAE. As of the latest updates, this compound is a research-grade chemical for ADC development and has not yet been approved for clinical use. It is not an approved drug.
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| Molecular Formula |
C29H29F4N5O4
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|---|---|
| Molecular Weight |
587.565280675888
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| Exact Mass |
587.216
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| CAS # |
2567724-20-1
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| PubChem CID |
172878672
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
42
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| Complexity |
808
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C(F)(F)(F)C(=O)O.C([C@H]1C[C@@H]1C1=CN=CC=C1)(=O)NC1C=CC(CNC(C2C=CC(N3CCNCC3)=CC=2)=O)=C(F)C=1
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| InChi Key |
SLGTZROYPZTPLC-ITNPDYSASA-N
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| InChi Code |
InChI=1S/C27H28FN5O2.C2HF3O2/c28-25-14-21(32-27(35)24-15-23(24)19-2-1-9-30-16-19)6-3-20(25)17-31-26(34)18-4-7-22(8-5-18)33-12-10-29-11-13-33;3-2(4,5)1(6)7/h1-9,14,16,23-24,29H,10-13,15,17H2,(H,31,34)(H,32,35);(H,6,7)/t23-,24+;/m1./s1
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| Chemical Name |
N-[[2-fluoro-4-[[(1S,2S)-2-pyridin-3-ylcyclopropanecarbonyl]amino]phenyl]methyl]-4-piperazin-1-ylbenzamide;2,2,2-trifluoroacetic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (Infinity mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (Infinity mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (Infinity mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7019 mL | 8.5096 mL | 17.0192 mL | |
| 5 mM | 0.3404 mL | 1.7019 mL | 3.4038 mL | |
| 10 mM | 0.1702 mL | 0.8510 mL | 1.7019 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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