NSC 663284
- Product Name
- NSC 663284
- CAS No.
- 383907-43-5
- Chemical Name
- NSC 663284
- Synonyms
- NSC 663284 (DA3003-1);CDC25 Phosphatase Inhibitor II, NSC 663284;5,8-Quinolinedione, 6-chloro-7-[[2-(4-morpholinyl)ethyl]amino]-;CDC25 Phosphatase Inhibitor II, NSC 663284 - CAS 383907-43-5 - Calbiochem
- CBNumber
- CB1504040
- Molecular Formula
- C15H16ClN3O3
- Formula Weight
- 321.76
- MOL File
- 383907-43-5.mol
NSC 663284 Property
- Boiling point:
- 478.8±45.0 °C(Predicted)
- Density
- 1.41±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMSO: 16 mg/mL
- form
- solid
- pka
- 6.79±0.10(Predicted)
- color
- red
- Sensitive
- Light Sensitive
- Stability:
- Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P405Store locked up.
N-Bromosuccinimide Price
- Product number
- N7537
- Product name
- NSC 663284
- Purity
- ≥98% (HPLC), solid
- Packaging
- 5mg
- Price
- $236
- Updated
- 2024/03/01
- Product number
- 217692
- Product name
- CDC25 Phosphatase Inhibitor II, NSC 663284
- Packaging
- 5mg
- Price
- $272
- Updated
- 2024/03/01
- Product number
- J66520
- Product name
- NSC 663284
- Packaging
- 1mg
- Price
- $66.5
- Updated
- 2023/06/20
- Product number
- J66520
- Product name
- NSC 663284
- Packaging
- 10mg
- Price
- $420
- Updated
- 2023/01/06
- Product number
- 13303
- Product name
- NSC 663284
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $25
- Updated
- 2024/03/01
NSC 663284 Chemical Properties,Usage,Production
Description
NSC663284 (383907-43-5) is a potent, selective and irreversible inhibitor of CDC25 phosphatases, Ki=29, 95 and 89 nM for human CDC25A, B2 and C respectively and >20- and >450-fold selective over VHR and PTP1B.1?Arrests cells at G1 and G2/M and inhibits cdk1 and 2 activation.2 Inhibits the growth of a variety of human tumor cell lines.3 NSC663284 acts via irreversible oxidation of the catalytic cysteine of CDC25.4
Uses
CDC25 Phosphatase Inhibitor II, NSC 663284 is a competitive CDC25 inhibitor and cell cycle arresting compound.
Definition
ChEBI: 6-chloro-7-[2-(4-morpholinyl)ethylamino]quinoline-5,8-dione is a quinolone.
General Description
A cell-permable, potent, irreversible, and competitive inhibitor of the Cdc25 phosphatase family (Ki = 29 nM, 95 nM, and 89 nM for Cdc25A, Cdc25B2, and Cdc25C, respectively) with anti-proliferative properties. Displays nearly 20- and 450-fold greater selectivity over VHR and PTP1B (IC50 = 4.0 μM and >100 μM, respectively). Reported to arrest cell cycle progression, inhibit Cdk dephosphorylation, and delay tumor growth (mean IC50 = 1.5 μM in NCI-60 tumor cell panel). Also shown to block ERK dephosphorylation caused by ectopic Cdc25A expression.
Biological Activity
Potent, selective inhibitor of Cdc25 dual specificity phosphatases (K i values are 29, 95 and 89 nM for human Cdc25A, Cdc25B 2 and Cdc25C respectively); > 20- and > 450-fold selective over VHR and PTP1B phosphatases respectively. Arrests cells at both G 1 and G 2 /M phase and blocks cdk2 and cdk1 activation. Blocks proliferation of a range of human tumor cell lines (IC 50 = 0.2-35 μ M).
Biochem/physiol Actions
Cell permeable: yes
storage
Store at +4°C
References
1) Lazo et al. (2001), Discovery and biological evaluation of a new family of potent inhibitors of the dual specificity protein phosphatases Cdc25; J. Med. Chem., 44 4042 2) Pu et al. (2002), Dual G1 and G2 phase inhibition by a novel, selective Cdc25 inhibitor 6-chloro-7-(2-morpholin-4-ylethylamino)-quinoline-3,8-dione; J. Biol. Chem., 277 46877 3) Han et al. (2004), NAD(P)H:quinone oxidoreductase-1-dependent and independent cytotoxicity of potent quinone Cdc25 phosphatase inhibitors; J. Pharmacol. Exp. Ther., 309 64 4) Brisson et al. (2005), Redox regulation of Cdc25B by cell-active quinolonediones; Mol. Pharmacol., 68 1810
NSC 663284 Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from NSC 663284 manufacturers
- Product
- NSC 663284 383907-43-5
- Price
- US $1500.00/g
- Min. Order
- 1g
- Purity
- 98%+
- Supply Ability
- 10
- Release date
- 2023-05-17