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- 详细信息
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
NSC 663284
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
383907-43-5
- 规格：
50mg/25mg/10mg/5mg/2mg
| 规格： | 50mg | 产品价格： | ￥3790.0 |
|---|---|---|---|
| 规格： | 25mg | 产品价格： | ￥2190.0 |
| 规格： | 10mg | 产品价格： | ￥1340.0 |
| 规格： | 5mg | 产品价格： | ￥890.0 |
| 规格： | 2mg | 产品价格： | ￥440.0 |
| 基本信息 | |
| CAS | No.383907-43-5 |
| 英文名称 | NSC 663284 |
| 别名 | DA-3003-1 |
| 分子式 | C15H16ClN3O3 |
| 分子量 | 321.76 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD08276924 |
| SMILES | C1COCCN1CCNC2=C(C(=O)C3=C(C2=O)N=CC=C3)Cl |
| InChIKey | BMKPVDQDJQWBPD-UHFFFAOYSA-N |
| InChI | InChI=1S/C15H16ClN3O3/c16-11-13(18-4-5-19-6-8-22-9-7-19)15(21)12-10(14(11)20)2-1-3-17-12/h1-3，18H，4-9H2 |
| PubChem CID | 379077 |
| 靶点 | Cdc25 dual specificity phosphatase;NSD2 |
| 通路 | Metabolic Enzyme&Protease |
| 背景说明 | NSC 663284 是一种有效的，细胞可渗透的且不可逆的 Cdc25 dual specificity phosphatase 抑制剂。NSC 663284 通过与 SET 结构域的相互作用来抑制 NSD2酶的活性。 |
| 生物活性 | 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 | IC50: 0.21 μM (Cdc25B2)[1] |
| In Vitro | We experimentally examined the 1990 compound National Cancer Institute Diversity Set and then computationally selected from their 140 000 compound repository 30 quinolinediones of which 8 had in vitro mean inhibitory concentrations <1 microM. The most potent was 6-chloro-7-(2-morpholin-4-ylethylamino)quinoline-5，8-dione (NSC 663284)， which was 20- and 450-fold more selective against Cdc25B(2) as compared with VHR or PTP1B phosphatases， respectively. NSC 663284 exhibited mixed competitive kinetics against Cdc25A， Cdc25B(2)， and Cdc25C with K(i) values of 29， 95， and 89 nM， respectively. As compared with NSC 663284， the regioisomer 7-chloro-6-(2-morpholin-4-ylethylamino)quinoline-5，8-dione was 3-fold less active against Cdc25B(2) in vitro and less potent as a growth inhibitor of human breast Cancer cells. Computational electrostatic potential mapping suggested the need for an electron-deficient 7-position for maximal inhibitor activity. Using a chemical complementation assay， we found that NSC 663284 blocked cellular ERK dephosphorylation caused by ectopic Cdc25A expression.[1]。 |
| 细胞实验 | In this study， the efficacy， pharmacokinetics， and metabolism of a potent quinolinedione Cdc25 Phosphatase Inhibitor， DA3003-1， in mice was examined. DA3003-1 inhibited the growth of subcutaneous human colon HT29 xenografts in SCID mice. After a single i.v. dose of 5 mg/kg， DA3003-1 was not detectable in plasma or tissues beyond 5 min. In vitro studies showed that DA3003-1 was rapidly dechlorinated and conjugated to glutathione. Following DA3003-1 treatment of tumor-bearing SCID mice， reduced glutathione concentrations in HT29 tumor were decreased to a greater extent and remained decreased for longer than the reduced glutathione concentrations in liver and kidneys. These studies suggest that the minimal antitumor activity of DA3003-1 in mice may be due to its rapid metabolism.[3]。 |
| 动物实验 | 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]. |
| 数据来源文献 | [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. [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. [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. |
| 单位 | 瓶 |
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IN3410 NSC 663284 代谢酶/蛋白酶 索莱宝
￥440 - 3790
