NSC 663284
Based on 6 publication(s) in Google Scholar
NSC 663284 (DA-3003-1) is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC50 for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively. NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM).
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- Pureté: 99.29%
- CAS No.: 383907-43-5
- Formule: C15H16ClN3O3
- Masse moléculaire:321.76
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) NSC 663284
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Customer Validation & Images
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Flow Cytometry
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Cell Proliferation/Viability Assay
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WB
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Cell Imaging/Staining
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Bio/Physico-chemical Assay
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Activité biologique
IC50: 0.21 μM (Cdc25B2)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
2.76 μM
Compound: NSC 663284
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Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
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[PMID: 31541869] |
| CEM-SS | CC50 |
2 μM
Compound: 663284
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Cytotoxicity in human CEM-SS cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity in human CEM-SS cells assessed as reduction in cell viability after 48 hrs by MTT assay
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[PMID: 27663546] |
| DLD-1 | IC50 |
>2 μM
Compound: 6a; NSC663284
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Cytotoxicity against human DLD1 cells assessed as growth inhibition after 72 hrs by MTS assay
Cytotoxicity against human DLD1 cells assessed as growth inhibition after 72 hrs by MTS assay
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[PMID: 37302341] |
| DU-145 | IC50 |
2.3 μM
Compound: 1, NSC-663284
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Antiproliferative activity against human androgen-independent prostate carcinoma DU145 cell line by colorimetric assay
Antiproliferative activity against human androgen-independent prostate carcinoma DU145 cell line by colorimetric assay
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[PMID: 16216500] |
| HEK-293T | CC50 |
13 μM
Compound: 663284
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Cytotoxicity in HEK293T cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity in HEK293T cells assessed as reduction in cell viability after 48 hrs by MTT assay
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[PMID: 27663546] |
| KB | IC50 |
4.89 μM
Compound: NSC 663284
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Antiproliferative activity against human KB cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
Antiproliferative activity against human KB cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
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[PMID: 31541869] |
| KMS-11 | IC50 |
1.43 μM
Compound: 6; DA3003-1
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Antiproliferative activity against human KMS-11 cells assessed as inhibition of cell growth incubated for 6 days by CCK-8 assay
Antiproliferative activity against human KMS-11 cells assessed as inhibition of cell growth incubated for 6 days by CCK-8 assay
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[PMID: 36642961] |
| MCF7 | IC50 |
1 μM
Compound: NSC 663284
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Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
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[PMID: 31541869] |
| MDA-MB-231 | IC50 |
>2 μM
Compound: 6a; NSC663284
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Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTS assay
Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTS assay
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[PMID: 37302341] |
| MDA-MB-231 | IC50 |
4.97 μM
Compound: NSC 663284
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Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
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[PMID: 31541869] |
| MIA PaCa-2 | IC50 |
2.5 μM
Compound: 1, NSC-663284
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Antiproliferative activity against human pancreatic carcinoma Mia PaCa2 cell line by colorimetric assay
Antiproliferative activity against human pancreatic carcinoma Mia PaCa2 cell line by colorimetric assay
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[PMID: 16216500] |
| MT4 | CC50 |
6 μM
Compound: 663284
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Cytotoxicity in human MT4 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity in human MT4 cells assessed as reduction in cell viability after 48 hrs by MTT assay
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[PMID: 27663546] |
| U2OS | CC50 |
270 nM
Compound: 12; DA3003-1
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Cytotoxicity against human U2OS cells assessed as cell growth inhibition
Cytotoxicity against human U2OS cells assessed as cell growth inhibition
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[PMID: 37578463] |
NSC 663284 (3-100μM; 48 hours) has a mean IC50 value in the NCI 60 Cell human tumor panel of 1.5 ± 0.6 μM, has IC50 values of 0.2 μM in human breast cancer MDA-MB-435 and MDA-N cells, has an IC50 value of 1.7 μM in human breast MCF-7 cells in culture[1]. NSC 663284 has relative IC50 values for Cdc25B2 (IC50=0.21 μM) are 20- and 450-fold lower than for VHR (IC50=4.0 μM) or PTP1B (IC50>4.0 μM), respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 383907-43-5
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Appearance Solid
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Masse moléculaire 321.76
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Formule C15H16ClN3O3
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Color Pink to red
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SMILES
O=C(C(Cl)=C1NCCN2CCOCC2)C3=C(N=CC=C3)C1=O
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Synonyms
DA-3003-1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (6)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
2025 Apr 11;16(1):276. PMID: 40216745
NSC 663284 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Apr 11;16(1):276. [Abstract]
Cell cycle assays were performed to evaluate the effects of varying concentrations of NSC663284 (1, 3, 5 μM) on A375 cells.
NSC 663284 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Apr 11;16(1):276. [Abstract]
CCK-8 assays demonstrated that NSC663284 (1, 3, 5 μM)-induced CDC25A inhibition suppressed proliferation in A375 and MUM2B cells.
NSC 663284 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Apr 11;16(1):276. [Abstract]
Increased phosphorylation of CDK1/2 was detected by western blot, confirming that NSC663284 (0.5, 0.75, 1 μM) effectively inhibited the function of CDC25A phosphatase in A375 and MUM2B
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Life Sci
Drug repurposing reveals Fmoc-l-leucine as an adipose thermogenesis activator in cold-exposed mice by targeting PPARγ/UCP1. [Abstract]2026 Apr 1:390:124259. PMID: 41655780 -
Commun Biol
Three-dimensional CRISPR screening reveals epigenetic interaction with anti-angiogenic therapy. [Abstract]2021 Jul 15;4(1):878. PMID: 34267311 -
Mol Cancer Res
Inhibition of the ATR-CHK1 Pathway in Ewing Sarcoma Cells Causes DNA Damage and Apoptosis via the CDK2-Mediated Degradation of RRM2. [Abstract]2020 Jan;18(1):91-104. PMID: 31649026 -
Bioengineered
CDC25C is a prognostic biomarker and correlated with mitochondrial homeostasis in pancreatic adenocarcinoma. [Abstract]2022 May;13(5):13089-13107. PMID: 35615982
NSC 663284 purchased from MedChemExpress. Usage Cited in: Bioengineered. 2022 May;13(5):13089-13107. [Abstract]
The impacts of CDC25C on the DNA synthesis through EdU assay after the treatment of NSC663284 and NSC95397 for 24 h.
NSC 663284 purchased from MedChemExpress. Usage Cited in: Bioengineered. 2022 May;13(5):13089-13107. [Abstract]
SW1990 cells were exposed to NSC663284 (0, 2.5, 5 μM) for 6 h, then the relative level of GSH was measured.
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Cell Signal
METTL3 contributes to osimertinib resistance in non-small cell lung cancer cell lines by regulating CDC25A and AURKB mRNA stability. [Abstract]2025 Oct 1:136:112156. PMID: 41043761
Solvant et solubilité
DMSO : ≥ 100 mg/mL (310.79 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.77 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.77 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
Mice: C.B.-17 SCID mice bearing HT29 human colon carcinoma xenografts are stratified into the following groups of 9-10 animals: Control, vehicle control, positive control (gemcitabine, 50 mg/kg/dose i.v.), NSC 663284 at the following doses: 2, 3 or 5 mg/kg/dose i.v.. The mice are dosed every 4 days for 6 doses, and body weights and tumor volumes are recorded twice weekly. Tumors are measured with calipers, and tumor volumes are calculated. Mice are followed for 3 weeks following the completion of the dosing to monitor tumor regrowth. In a second study, C.B.-17 SCID mice bearing MDA-MB-435 human breast cancer xenografts are stratified to the same treatment groups, except that paclitaxel at 20 mg/kg i.v. every 7 days is used as the positive control[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Lazo JS, et al. Discovery and biological evaluation of a new family of potent inhibitors of the dual specificity protein phosphatase Cdc25. J Med Chem. 2001 Nov 22;44(24):4042-9. [Content Brief]
[2]. Coussens NP, et al. High-throughput screening with nucleosome substrate identifies small-molecule inhibitors of the human histone lysine methyltransferase NSD2. J Biol Chem. 2018 Aug 31;293(35):13750-13765. [Content Brief]
[3]. Guo J, et al. Pharmacology and antitumor activity of a quinolinedione Cdc25 phosphatase inhibitor DA3003-1 (NSC 663284). Anticancer Res. 2007 Sep-Oct;27(5A):3067-73. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1079 mL | 15.5395 mL | 31.0791 mL | 77.6977 mL |
| 5 mM | 0.6216 mL | 3.1079 mL | 6.2158 mL | 15.5395 mL | |
| 10 mM | 0.3108 mL | 1.5540 mL | 3.1079 mL | 7.7698 mL | |
| 15 mM | 0.2072 mL | 1.0360 mL | 2.0719 mL | 5.1798 mL | |
| 20 mM | 0.1554 mL | 0.7770 mL | 1.5540 mL | 3.8849 mL | |
| 25 mM | 0.1243 mL | 0.6216 mL | 1.2432 mL | 3.1079 mL | |
| 30 mM | 0.1036 mL | 0.5180 mL | 1.0360 mL | 2.5899 mL | |
| 40 mM | 0.0777 mL | 0.3885 mL | 0.7770 mL | 1.9424 mL | |
| 50 mM | 0.0622 mL | 0.3108 mL | 0.6216 mL | 1.5540 mL | |
| 60 mM | 0.0518 mL | 0.2590 mL | 0.5180 mL | 1.2950 mL | |
| 80 mM | 0.0388 mL | 0.1942 mL | 0.3885 mL | 0.9712 mL | |
| 100 mM | 0.0311 mL | 0.1554 mL | 0.3108 mL | 0.7770 mL |
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