NSC 663284 (Synonyms: DA-3003-1)

目录号: HY-100034 纯度: 99.79%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

NSC 663284 (DA-3003-1) 是一种有效的，细胞可渗透的且不可逆的 Cdc25 dual specificity phosphatase 抑制剂，Cdc25B₂ 的 IC₅₀ 为 0.21 μM。NSC 663284 表现出与 Cdc25A，Cdc25B₂ 和 Cdc25C 的混合竞争动力学，Ki 值分别为 29、95 和 89 nM。NSC 663284 通过与 SET 结构域 (K_d of 370 nM) 的相互作用来抑制 NSD2 (IC₅₀ of 170 nM) 酶的活性。

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NSC 663284 Chemical Structure

CAS No. : 383907-43-5

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥990	In-stock
2 mg	￥450	In-stock
5 mg	￥900	In-stock
10 mg	￥1350	In-stock
25 mg	￥2200	In-stock
50 mg	￥3800	In-stock
100 mg	现货	询价
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

MCE 顾客使用本产品发表的 3 篇科研文献

NSC 663284 相关产品

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查看 Histone Methyltransferase 亚型特异性产品:

查看所有亚型

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

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

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]

细胞效力
(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]

体外研究
(In Vitro)

NSC 663284 (3-100 μM；48 小时) 在 NCI 60 细胞人类肿瘤组中的平均 IC₅₀ 值为 1.5 ± 0.6 μM，在人乳腺癌 MDA-MB-435 和 MDA-N 细胞中的 IC₅₀ 值为 0.2 μM，在培养的人乳腺 MCF-7 细胞中的 IC₅₀ 值为 1.7 μM^[1]。
NSC 663284 对 Cdc25B2 的相对 IC₅₀ 值 (IC₅₀=0.21 μM) 比 VHR (IC_{低 20 倍和 450 倍>50}=4.0 μM) 或 PTP1B (IC₅₀>4.0 μM)^[1]。

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

体内研究
(In Vivo)

NSC 663284 (静脉注射；2、3 和 5mg/kg) 抑制 SCID 小鼠皮下人结肠 HT29 异种移植物的生长。单剂量 5 mg/kg 后，NSC 663284 在血浆或组织中检测不到超过 5 分钟。在 NSC 663284 处理荷瘤 SCID 小鼠后，HT29 肿瘤中谷胱甘肽浓度的降低幅度更大，并且比肝脏和肾脏中谷胱甘肽浓度降低的时间更长^[3]。

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

分子量

321.76

Formula

C₁₅H₁₆ClN₃O₃

CAS 号

383907-43-5

性状

固体

颜色

Pink to red

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 100 mg/mL (310.79 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	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

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

摩尔计算器
稀释计算器

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

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.77 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.77 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.77 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.79%

选择批次：

Data Sheet (644 KB) SDS (251 KB)

COA (191 KB) RP-HPLC (248 KB)

产品使用指南 (1538 KB)

参考文献

[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. [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.
参考文献	[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. [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.

参考文献

[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. [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]

NSC 663284 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	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

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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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

NSC 663284 (Synonyms: DA-3003-1)

Customer Review

MCE 顾客使用本产品发表的 3 篇科研文献