| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
NSC348884 is a brand-new and powerful nucleophosmin inhibitor that can disrupt oligomer formation and trigger apoptosis. With an IC50 range of 1.7–4.0 μM against cell proliferation in various cancer cell lines.
| Targets |
LNCaP cells (IC50 = 4 μM); Granta cells (IC50 = 1.7 μM)
Nucleophosmin/B23 (NPM/B23) inhibitor [1] |
|---|---|
| ln Vitro |
NSC348884 (0-6 μM; 24 h) binds to NPM and prevents NPM oligomerization[1].
NSC348884 (0.01-100 μM; 4 d) shows cytotoxicity to cancer cells[1]. NSC348884 (1 μM; 4 d) exhibits cytotoxicity against mantle cell lymphoma[1]. NSC348884 (1-5 μM; 24 h) induces cell apoptosis[1]. NSC348884 (0-5 μM; 0-24 h) upregulates the level of p53[1]. Treatment of human ovarian cancer cells (SKOV3, ES2) and murine ovarian cancer cells (MOSEC/Luc) with NSC348884 at concentrations of 2.5 μM and 5 μM for 48 hours resulted in a dose-dependent increase in PD-L1 protein expression as detected by Western blot analysis. [1] Flow cytometry analysis confirmed that NSC348884 treatment (0, 2.5, 5 μM for 48h) significantly increased the surface expression of PD-L1 on SKOV3, ES2, and MOSEC/Luc cells. [1] NSC348884 disrupts the formation of NPM/B23 oligomers and suppresses their function in cancer cells. [1] |
| ln Vivo |
NSC348884 (50 μg; i.p. once) reduces tumor growth[2].
In an immunocompetent C57Bl/6J mouse model bearing MOSEC/Luc tumors, intraperitoneal administration of NSC348884 (50 μg per mouse, once weekly) significantly reduced tumor growth compared to the vehicle control group, as monitored by bioluminescence imaging. [1] Tumors excised from mice treated with NSC348884 showed increased PD-L1 expression compared to tumors from the control group. [1] The combination of NSC348884 (50 μg, i.p., weekly) and an anti-PD-1 antibody (100 μg, i.p., weekly) demonstrated superior antitumor efficacy compared to either monotherapy. This combination significantly reduced tumor growth, increased the infiltration of cytotoxic CD8+ T cells into tumors, reduced ascites formation, and markedly prolonged the overall survival of tumor-bearing mice. [1] |
| Cell Assay |
For Western blot analysis to assess PD-L1 expression, cells were harvested, washed, and lysed in ice-cold RIPA buffer. Lysates were boiled in SDS sample buffer, separated by SDS-PAGE, and transferred to a nitrocellulose membrane. Membranes were then probed with primary antibodies against PD-L1 and β-actin, followed by appropriate secondary antibodies. [1]
For flow cytometry analysis of PD-L1 surface expression, cells were stained with PD-L1-APC antibody or corresponding isotype control, and analyzed using a flow cytometer. Data analysis was performed using dedicated software. [1] Cells (SKOV3, ES2, MOSEC/Luc) were exposed to NSC348884 at specified concentrations (0, 2.5, 5 μM) for 48 hours before analysis. [1] |
| Animal Protocol |
To evaluate the antitumor activity of NSC348884 alone or in combination, MOSEC/Luc cells were harvested and resuspended. Tumors were established in 6-8 week-old immunocompetent C57Bl/6J mice by intraperitoneal inoculation of the cell suspension. [1]
After tumor establishment (7-14 days), mice were randomized into treatment groups. NSC348884 was administered intraperitoneally at a dose of 50 μg per mouse, once weekly. The anti-PD-1 antibody was administered intraperitoneally at 100 μg per mouse, once weekly. The control group received an isotype control antibody. [1] Tumor growth was monitored weekly using an in vivo imaging system to measure luciferase activity. Body weight was monitored, and ascites volume was measured upon sacrifice. Survival was recorded. [1] |
| References | |
| Additional Infomation |
NSC348884 has been identified as an inhibitor/regulator of nucleolar phosphoprotein (NPM/B23). [1] In ovarian cancer, NSC348884 inhibits tumorigenesis and increases PD-L1 expression. This study suggests that targeting NPM/B23 with NSC348884 may enhance the sensitivity of ovarian cancer cells to immunotherapy with PD-1 inhibitors. [1] The mechanism involves NPM/B23 negatively regulating PD-L1 expression by stabilizing the NF-κB/p65 protein complex and interfering with the IFN-γ-dependent signaling pathway. Inhibition of NPM/B23 by NSC348884 leads to increased PD-L1 expression, and the combination of increased PD-L1 with PD-1 blockade may enhance the anti-tumor immune response. [1]
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| Molecular Formula |
C38H40N10
|
|---|---|
| Molecular Weight |
636.7912
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| Exact Mass |
636.343
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| Elemental Analysis |
C, 71.67; H, 6.33; N, 22.00
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| CAS # |
81624-55-7
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| Related CAS # |
81624-55-7
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| PubChem CID |
335974
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| Appearance |
Solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
1001.7±65.0 °C at 760 mmHg
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| Flash Point |
559.6±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.768
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| LogP |
4.74
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
48
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| Complexity |
891
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1=C(CN(CCN(CC2NC3C(=CC(C)=CC=3)N=2)CC2NC3C(=CC(C)=CC=3)N=2)CC2NC3C(=CC(C)=CC=3)N=2)NC2C1=CC=C(C)C=2
|
| InChi Key |
KZOLQEUQAFTQFM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C38H40N10/c1-23-5-9-27-31(15-23)43-35(39-27)19-47(20-36-40-28-10-6-24(2)16-32(28)44-36)13-14-48(21-37-41-29-11-7-25(3)17-33(29)45-37)22-38-42-30-12-8-26(4)18-34(30)46-38/h5-12,15-18H,13-14,19-22H2,1-4H3,(H,39,43)(H,40,44)(H,41,45)(H,42,46)
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| Chemical Name |
N,N,N',N'-tetrakis[(6-methyl-1H-benzimidazol-2-yl)methyl]ethane-1,2-diamine
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| Synonyms |
NSC348884; NSC 348884; NSC-348884
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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: 34~100 mg/mL (53.4~157.0 mM)
Ethanol: ~100 mg/mL (~157.0 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (3.93 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (3.93 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 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 (3.93 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 | 1.5704 mL | 7.8519 mL | 15.7038 mL | |
| 5 mM | 0.3141 mL | 1.5704 mL | 3.1408 mL | |
| 10 mM | 0.1570 mL | 0.7852 mL | 1.5704 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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