1. Metabolic Enzyme/Protease
  2. Phosphatase

NSC 663284 (Synonyms: DA-3003-1)

Cat. No.: HY-100034 Purity: >98.0%
Handling Instructions

NSC 663284 is a Cdc25 dual specificity phosphatases inhibitor with an IC50 of 0.21 μM.

For research use only. We do not sell to patients.
NSC 663284 Chemical Structure

NSC 663284 Chemical Structure

CAS No. : 383907-43-5

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 106 In-stock
2 mg USD 60 In-stock
5 mg USD 108 In-stock
10 mg USD 192 In-stock
25 mg USD 396 In-stock
50 mg USD 708 In-stock
100 mg USD 1194 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

NSC 663284 is a Cdc25 dual specificity phosphatases inhibitor with an IC50 of 0.21 μM.

IC50 & Target

IC50: 0.21 μM (Cdc25 dual specificity phosphatase)[1]

In Vitro

The Cdc25 dual specificity phosphatases have central roles in coordinating cellular signaling processes and cell proliferation. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B2, and Cdc25C with Ki values of 29, 95, and 89 nM, respectively. NSC 663284 blocks cellular Erk dephosphorylation caused by ectopic Cdc25A expression. NSC 663284 displays a strong preference for Cdc25B2 as compared with VHR or PTP1B, the relative IC50 values for Cdc25B2 are 20- and 450-fold lower than for VHR or PTP1B, respectively. NSC 663284 blocks cell proliferation and the actions of cellular cdc25a. NSC 663284 has a mean IC50 value in the NCI 60 Cell Human Tumor Panel of 1.5 (0.6 µM when cells are treated for 48 h). Most sensitive are human breast cancer MDA-MB-435 and MDA-N cells, which have IC50 values of 0.2 µM[1].

In Vivo

NSC 663284 inhibits the growth of subcutaneous human colon HT29 xenografts in SCID mice. After a single i.v. 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[2].

References
Preparing Stock Solutions
Concentration Volume 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.
Animal Administration
[2]

NSC 663284 is prepared in dextrose (5%) for injection.

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
Molecular Weight

321.76

Formula

C₁₅H₁₆ClN₃O₃

CAS No.

383907-43-5

SMILES

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥150 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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