| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg | |||
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| Other Sizes |
| Targets |
CB-30865 targets nicotinamide phosphoribosyltransferase (Nampt). Nampt is a critical enzyme in the NAD+ salvage pathway. By inhibiting Nampt, CB-30865 depletes intracellular NAD+ levels. This has a profound effect on cellular metabolism, as NAD+ is a cofactor for many enzymes, including sirtuins and PARPs. The depletion of NAD+ leads to a decrease in ATP production, ultimately resulting in cell death, particularly in cancer cells that are highly dependent on this pathway.
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| ln Vitro |
By inhibiting Nampt, CB30865 reduces NAD and demonstrates cytotoxicity [1].
CB-30865 is a highly potent growth inhibitory agent. In vitro, it demonstrates IC50 values in the range of 1-100 nM for several mouse and human cell types. It is a potent inhibitor of Nampt, and its cellular toxicity is a direct result of NAD+ depletion. The compound is highly effective against a range of human tumor cell lines, with IC50 values in the 1-10 nM range. Its potency is attributed to its ability to effectively inhibit the Nampt enzyme. |
| ln Vivo |
While CB-30865 is primarily studied in vitro, its mechanism of action suggests that it would have potent antitumor activity in vivo. As an inhibitor of Nampt, it would deplete NAD+ in tumor cells, leading to energy crisis and cell death. However, specific in vivo data is not detailed in the provided sources. The compound is used as a research tool to study the role of NAD+ metabolism in cancer and other diseases.
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| Enzyme Assay |
The in vitro activity of CB-30865 against Nampt is determined using enzyme activity assays. In a typical protocol, recombinant Nampt is incubated with its substrates (nicotinamide and ATP) in the presence or absence of the compound. The production of nicotinamide mononucleotide (NMN), the product of the reaction, is then measured. The IC50, the concentration of CB-30865 that inhibits 50% of the enzyme activity, is calculated. This assay directly measures the compound's potency against its primary target.
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| Cell Assay |
The in vitro cellular activity of CB-30865 is assessed using cell viability and proliferation assays. In a standard protocol, cancer cells (e.g., W1L2 cells or other human tumor cell lines) are seeded in 96-well plates and treated with increasing concentrations of CB-30865 for a period (e.g., 48-72 hours). Cell viability is then measured. The IC50 or EC50 values are calculated to quantify the compound's potency. These assays demonstrate the compound's ability to inhibit cell growth in a cellular context.
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| Animal Protocol |
The in vivo efficacy of CB-30865 would be evaluated in xenograft mouse models. In these studies, human tumor cells are implanted into immunodeficient mice. When tumors reach a certain size, the animals are treated with CB-30865. Tumor growth is monitored by caliper measurements. These studies are essential for determining the compound's in vivo antitumor activity, pharmacokinetic properties, and therapeutic window.
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| ADME/Pharmacokinetics |
Dosing in animal models would typically involve intravenous or intraperitoneal administration, as small molecule inhibitors of Nampt are often administered parenterally. The compound would be formulated in a suitable vehicle for injection. Detailed pharmacokinetic data is not provided, but as a potent Nampt inhibitor, its properties would be characterized in drug development studies.
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| Toxicity/Toxicokinetics |
The toxicity profile of CB-30865 is likely related to its potent inhibition of Nampt and depletion of NAD+, which is essential for the viability of all cells. While cancer cells are particularly sensitive to NAD+ depletion, this approach can also affect normal cells, leading to potential toxicity. The compound is highly cytotoxic, indicating that it would have a narrow therapeutic window and require careful dosing to manage side effects.
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| References |
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| Additional Infomation |
CB-30865 is also known as ZM 242421. It is a potent and selective inhibitor of Nampt, a key enzyme in NAD+ biosynthesis. It has strong cytotoxic activity against a range of cancer cell lines. The compound is used as a research tool to study NAD+ metabolism and its role in cancer and other diseases. It represents a class of compounds that target cancer cell metabolism and has been investigated for its potential as an anticancer agent.
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| Molecular Formula |
C26H22BRN5O2
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|---|---|
| Molecular Weight |
516.399
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| Exact Mass |
515.096
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| CAS # |
206275-15-2
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| PubChem CID |
135528987
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| Appearance |
White to off-white solid powder
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| LogP |
4.762
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
34
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| Complexity |
815
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SHNBLWMBWXIKMR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H22BrN5O2/c1-3-11-32(16-20-12-22-24(13-23(20)27)30-17(2)31-26(22)34)21-8-6-19(7-9-21)25(33)29-15-18-5-4-10-28-14-18/h1,4-10,12-14H,11,15-16H2,2H3,(H,29,33)(H,30,31,34)
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| Chemical Name |
4-[(7-bromo-2-methyl-4-oxo-3H-quinazolin-6-yl)methyl-prop-2-ynylamino]-N-(pyridin-3-ylmethyl)benzamide
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| Synonyms |
CB30865 CB 30865 CB-30865
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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 |
| 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 : ~33.33 mg/mL (~64.54 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9365 mL | 9.6824 mL | 19.3648 mL | |
| 5 mM | 0.3873 mL | 1.9365 mL | 3.8730 mL | |
| 10 mM | 0.1936 mL | 0.9682 mL | 1.9365 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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