| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
CB-300919 targets nicotinamide phosphoribosyltransferase (NAMPT), an enzyme involved in NAD+ biosynthesis. NAMPT inhibition depletes cellular NAD+ levels, leading to ATP depletion and cell death in susceptible tumor cells. CB-300919 acts as a NAMPT inhibitor, interfering with metabolic pathways essential for tumor cell survival and proliferation.
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|---|---|
| ln Vitro |
CB-300919 demonstrates potent antitumor activity against the CH1 human ovarian tumor xenograft model. As a NAMPT inhibitor, it depletes NAD+ and induces metabolic stress in cancer cells. Detailed IC50 values in public literature are limited. The compound shows high activity in preclinical tumor models, supporting its development as an anticancer agent.
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| ln Vivo |
CB-300919 exhibits high in vivo activity in the CH1 human ovarian tumor xenograft model. It demonstrates antitumor efficacy through NAMPT inhibition and NAD+ depletion. The compound is used in preclinical cancer research for NAMPT-dependent malignancies.
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| Enzyme Assay |
NAMPT enzyme assay: incubate recombinant NAMPT with nicotinamide, PRPP, and ATP in assay buffer. Add CB-300919 (0.1 nM-100 μM). Measure NAD+ production by spectrophotometric or fluorometric methods. Calculate IC50 values by nonlinear regression.
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| Cell Assay |
Cell viability assay: culture NAMPT-sensitive cancer cell lines (e.g., CH1 ovarian cells) in appropriate medium. Seed into 96-well plates and treat with CB-300919 (0.1 nM-100 μM) for 48-72 h. Measure cell viability by MTT or CellTiter-Glo. Determine IC50 values.
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| Animal Protocol |
Xenograft tumor model: inoculate nude mice with CH1 human ovarian tumor cells subcutaneously. When tumors reach measurable size, administer CB-300919 by intraperitoneal or intravenous injection at various doses and schedules. Monitor tumor volume and body weight. Assess tumor growth inhibition and NAD+ levels in tumor tissue.
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| References |
| Molecular Formula |
C32H34CLN7O2
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|---|---|
| Molecular Weight |
584.11
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| Exact Mass |
583.246
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| CAS # |
289715-28-2
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| PubChem CID |
9938280
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| Appearance |
White to off-white solid powder
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| LogP |
3.565
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
42
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| Complexity |
1010
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1CCN(CC1)CC2=NC3=C(C(N2C)=O)C=C(CN(CC#C)C4=CC=C(C=C4)C(NCC5=CC=CN=C5)=O)C(Cl)=C3
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| InChi Key |
LWTCFUSGPRGUBX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H34ClN7O2/c1-4-12-40(26-9-7-24(8-10-26)31(41)35-20-23-6-5-11-34-19-23)21-25-17-27-29(18-28(25)33)36-30(38(3)32(27)42)22-39-15-13-37(2)14-16-39/h1,5-11,17-19H,12-16,20-22H2,2-3H3,(H,35,41)
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| Chemical Name |
4-[[7-chloro-3-methyl-2-[(4-methylpiperazin-1-yl)methyl]-4-oxoquinazolin-6-yl]methyl-prop-2-ynylamino]-N-(pyridin-3-ylmethyl)benzamide
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| Synonyms |
CB 300919; CB300919; CB-300919
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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: ≥ 100 mg/mL (~171.20 mM)
H2O: < 0.1 mg/mL (Insoluble) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (5.14 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 30.0 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: 3 mg/mL (5.14 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 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: ≥ 3 mg/mL (5.14 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 | 1.7120 mL | 8.5600 mL | 17.1201 mL | |
| 5 mM | 0.3424 mL | 1.7120 mL | 3.4240 mL | |
| 10 mM | 0.1712 mL | 0.8560 mL | 1.7120 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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