NSC 663284 (Synonyms: DA-3003-1)

Name: NSC 663284
Brand: MedChemExpress
SKU: HY-100034
Rating: 5.0 (3 reviews)

Cat. No.: HY-100034 Purity: 99.79%: FAQs
Data Sheet SDS COA Handling Instructions

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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).

For research use only. We do not sell to patients.

NSC 663284 Chemical Structure

CAS No. : 383907-43-5

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 117	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 117	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 119	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 211	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 436	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 779	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1313	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

3 Publications Citing Use of MCE NSC 663284

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View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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]

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]
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]
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	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]

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.

Molecular Weight

321.76

Formula

C₁₅H₁₆ClN₃O₃

CAS No.

383907-43-5

Appearance

Solid

Color

Pink to red

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.79%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (247 KB) RP-HPLC (248 KB)

Handling Instructions (2659 KB)

References

[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]

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].

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

References

[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

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

NSC 663284 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NSC 663284383907-43-5DA-3003-1NSC663284NSC-663284PhosphataseHistone MethyltransferaseInhibitorinhibitorinhibit

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NSC 663284 (Synonyms: DA-3003-1)

Customer Review

NSC 663284 Related Antibodies

3 Publications Citing Use of MCE NSC 663284

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•Related Screening Libraries:

•Related Small Molecules:

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View All Histone Methyltransferase Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

NSC 663284 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

NSC 663284 Related Classifications

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