Referencia número: HY-100034

NSC 663284

(Synonyms: DA-3003-1)

6 Cited Publications

Revisión del cliente

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 (K_d of 370 nM).

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Pureza: 99.29%
No. CAS: 383907-43-5
Fòrmula: C₁₅H₁₆ClN₃O₃
Peso molecular:321.76

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

NSC 663284 Chemical Structure

No. CAS: 383907-43-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

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^[1]. NSC 663284 inhibits NSD2 (IC₅₀ of 170 nM) through a direct interaction with the catalytic SET domain (K_d of 370 nM)^[2].

IC₅₀ & Target

IC50: 0.21 μM (Cdc25B2)^[1]

Ver todos los productos específicos de isoformas Histone Methyltransferase :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	2.76 μM Compound: NSC 663284	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	[PMID: 31541869]
CEM-SS	CC₅₀	2 μM Compound: 663284	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	[PMID: 27663546]
DLD-1	IC₅₀	>2 μM Compound: 6a; NSC663284	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	[PMID: 37302341]
DU-145	IC₅₀	2.3 μM Compound: 1, NSC-663284	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	[PMID: 16216500]
HEK-293T	CC₅₀	13 μM Compound: 663284	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	[PMID: 27663546]
KB	IC₅₀	4.89 μM Compound: NSC 663284	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	[PMID: 31541869]
KMS-11	IC₅₀	1.43 μM Compound: 6; DA3003-1	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	[PMID: 36642961]
MCF7	IC₅₀	1 μM Compound: NSC 663284	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	[PMID: 31541869]
MDA-MB-231	IC₅₀	>2 μM Compound: 6a; NSC663284	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	[PMID: 37302341]
MDA-MB-231	IC₅₀	4.97 μM Compound: NSC 663284	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	[PMID: 31541869]
MIA PaCa-2	IC₅₀	2.5 μM Compound: 1, NSC-663284	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	[PMID: 16216500]
MT4	CC₅₀	6 μM Compound: 663284	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	[PMID: 27663546]
U2OS	CC₅₀	270 nM Compound: 12; DA3003-1	Cytotoxicity against human U2OS cells assessed as cell growth inhibition Cytotoxicity against human U2OS cells assessed as cell growth inhibition	[PMID: 37578463]

In Vitro

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.

In Vivo

NSC 663284 (intravenous injection; 2, 3, and 5mg/kg) inhibits the growth of subcutaneous human colon HT29 xenografts in SCID mice. After a single dose of 5 mg/kg, NSC 663284 is not detectable in plasma or tissues beyond 5 min. Following NSC 663284 treatment of tumor-bearing SCID mice, reduces glutathione concentrations in HT29 tumor are decreased to a greater extent and remained decreased for longer than the reduced glutathione concentrations in liver and kidneys^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

No. CAS 383907-43-5
Appearance Solid
Peso molecular 321.76
Fòrmula C₁₅H₁₆ClN₃O₃
Color Pink to red
SMILES

O=C(C(Cl)=C1NCCN2CCOCC2)C3=C(N=CC=C3)C1=O
Synonyms

DA-3003-1
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (6)

All Cell Imaging/StainingFlow CytometryBio/Physico-chemical AssayCell Proliferation/Viability AssayWB

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Cell Death Dis

CDC25A inhibition sensitizes melanoma cells to doxorubicin and NK cell therapy. [Abstract]

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
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.
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

Solvente y solubilidad

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.1079 mL

15.5395 mL

31.0791 mL

5 mM

0.6216 mL

3.1079 mL

6.2158 mL

10 mM

0.3108 mL

1.5540 mL

3.1079 mL

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.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.77 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protocolo

Animal Administration^[2]

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.

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (279 KB)
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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

NSC 663284

6 Cited Publications

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NSC 663284

Epigenetics Compound Library

Metabolism/Protease Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Phosphatase Inhibitor Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) NSC 663284

Ver todos los productos específicos de isoformas Histone Methyltransferase

Actividad biológica

Chemical Information

Publications (6)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

NSC 663284

Epigenetics Compound Library

Metabolism/Protease Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Phosphatase Inhibitor Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) NSC 663284

Ver todos los productos específicos de isoformas Histone Methyltransferase

Actividad biológica

Chemical Information

Publications (6)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

NSC 663284 Related Classifications

HY-100034 Related Classifications