1. Metabolic Enzyme/Protease
    Epigenetics
  2. Phosphatase
    Histone Methyltransferase
  3. NSC 663284

NSC 663284 (Synonyms: DA-3003-1)

Cat. No.: HY-100034 Purity: 99.87%
Handling Instructions

NSC 663284 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).

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

NSC 663284 Chemical Structure

NSC 663284 Chemical Structure

CAS No. : 383907-43-5

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
2 mg USD 60 In-stock
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5 mg USD 108 In-stock
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10 mg USD 192 In-stock
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25 mg USD 396 In-stock
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50 mg USD 708 In-stock
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100 mg USD 1194 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

NSC 663284 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 (Kd of 370 nM)[2].

IC50 & Target

IC50: 0.21 μM (Cdc25B2)[1]

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].

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].

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

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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 150 mg/mL (466.19 mM)

*"≥" 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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
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Keywords:

NSC 663284DA-3003-1NSC663284NSC-663284PhosphataseHistone MethyltransferaseInhibitorinhibitorinhibit

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Product Name:
NSC 663284
Cat. No.:
HY-100034
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