Navitoclax (Synonyms: ABT-263)

目录号: HY-10087 纯度: 99.72%: FAQs
Data Sheet SDS COA 产品使用指南技术支持

Navitoclax (ABT-263) 是一种口服有效的 Bcl-2 抑制剂，可与 Bcl-x_L，Bcl-2，Bcl-w 等多种 Bcl-2 家族蛋白结合，K_i 值小于 1 nM。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

Navitoclax Chemical Structure

CAS No. : 923564-51-6

1. 客户无需承担相应的运输费用。

2. 同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

可免费申领三个不同产品的试用装。

3. 试用装只面向终端客户。

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1029	In-stock
1 mg	￥291	In-stock
5 mg	￥650	In-stock
10 mg	￥960	In-stock
25 mg	￥1713	In-stock
50 mg	￥2500	In-stock
100 mg	￥3500	In-stock
200 mg	￥4950	In-stock
500 mg	现货	询价
1 g	现货	询价
5 g		询价
10 g		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Navitoclax:

Navitoclax-d₈ In-stock
Navitoclax dihydrochloride 询价

MCE 顾客使用本产品发表的 92 篇科研文献

Proliferation Assay

: Navitoclax purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Sep 24;9(10):986. [Abstract]; Cells are treated with 25 nM siRNA for 48 hours followed by 1 μM ABT-263 for 36 hours.

: Navitoclax purchased from MCE. Usage Cited in: ACS Med Chem Lett. 2015 Jun 22;6(8):948-52. [Abstract]; Combination treatment. (a) Comparison of AZD-8055 and ABT-263 treatment in all cell lines. Red indicates sensitivity, while blue indicates resistance. (b) Depiction of synergism where the values shown are excess over Bliss Independence, a prediction of inhibition without synergism. Increased synergism is evident by an increased number, shown in red, while negative numbers in blue represent an antagonistic effect.

Navitoclax 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Bcl-2 Family 亚型特异性产品:

查看所有亚型

Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

生物活性
纯度 & 产品资料
参考文献

生物活性

Navitoclax (ABT-263) is a potent and orally active Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-x_L, Bcl-2 and Bcl-w, with a K_i of less than 1 nM^[1].

IC₅₀ & Target^[1]

Bcl-W

1 nM (Ki)

Bcl-xL

1 nM (Ki)

Bcl-2

1 nM (Ki)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
FL5.12	EC₅₀	4.2 nM Compound: 2, ABT-263	Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl-XL assessed as cell viability after 24 hrs by MTS assay in absence of serum Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl-XL assessed as cell viability after 24 hrs by MTS assay in absence of serum	[PMID: 18841882]
FL5.12	EC₅₀	5.9 nM Compound: 2, ABT-263	Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl2 assessed as cell viability after 24 hrs by MTS assay in absence of serum Cytotoxicity against IL3-dependent mouse FL5.12 cells overexpressing human Bcl2 assessed as cell viability after 24 hrs by MTS assay in absence of serum	[PMID: 18841882]
MOLT-4	EC₅₀	0.3 μM Compound: 1; ABT-263	Cytotoxicity against human MOLT-4 cells assessed as reduction in cell viability measured after 48 hrs by celltiter-glo assay Cytotoxicity against human MOLT-4 cells assessed as reduction in cell viability measured after 48 hrs by celltiter-glo assay	[PMID: 34141086]
MOLT-4	IC₅₀	212.3 nM Compound: ABT-263	Cytotoxicity against human MOLT-4 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay Cytotoxicity against human MOLT-4 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay	[PMID: 34533954]
NCI-H1417	IC₅₀	54.2 nM Compound: 2, ABT-263	Cytotoxicity against human NCI-H1417 cells assessed as growth inhibition after 4 days by WST assay Cytotoxicity against human NCI-H1417 cells assessed as growth inhibition after 4 days by WST assay	[PMID: 23448298]
NCI-H146	EC₅₀	0.08 μM Compound: 2, ABT-263	Cytotoxicity against human NCI-H146 after 48 hrs by MTS assay in presence of 10% human serum Cytotoxicity against human NCI-H146 after 48 hrs by MTS assay in presence of 10% human serum	[PMID: 21366295]
NCI-H146	EC₅₀	86.7 nM Compound: 2, ABT-263	Cytotoxicity against human NCI-H146 cells assessed as cell viability after 48 hrs in presence of 10% human serum Cytotoxicity against human NCI-H146 cells assessed as cell viability after 48 hrs in presence of 10% human serum	[PMID: 18841882]
NCI-H187	IC₅₀	38.4 nM Compound: 2, ABT-263	Cytotoxicity against human NCI-H187 cells assessed as growth inhibition after 4 days by WST assay Cytotoxicity against human NCI-H187 cells assessed as growth inhibition after 4 days by WST assay	[PMID: 23448298]
NCI-H1963	EC₅₀	0.051 μM Compound: 2, ABT-263	Cytotoxicity against human NCI-H1963 after 48 hrs by MTS assay in presence of 10% human serum Cytotoxicity against human NCI-H1963 after 48 hrs by MTS assay in presence of 10% human serum	[PMID: 21366295]
NCI-H1963	IC₅₀	26.6 nM Compound: 2, ABT-263	Cytotoxicity against human NCI-H1963 cells assessed as growth inhibition after 4 days by WST assay Cytotoxicity against human NCI-H1963 cells assessed as growth inhibition after 4 days by WST assay	[PMID: 23448298]
NCI-H889	EC₅₀	0.12 μM Compound: 2, ABT-263	Cytotoxicity against human NCI-H889 after 48 hrs by MTS assay in presence of 10% human serum Cytotoxicity against human NCI-H889 after 48 hrs by MTS assay in presence of 10% human serum	[PMID: 21366295]
Platelet	IC₅₀	0.189 μM Compound: ABT-263	Cytotoxicity against human platelet assessed as cell viability measured after 72 hrs by MTS assay Cytotoxicity against human platelet assessed as cell viability measured after 72 hrs by MTS assay	[PMID: 32388279]
Platelet	IC₅₀	0.325 μM Compound: ABT-263	Cytotoxicity against platelets in human PRP assessed as reduction in cell viability measured after 48 hrs by MTS assay Cytotoxicity against platelets in human PRP assessed as reduction in cell viability measured after 48 hrs by MTS assay	[PMID: 34533954]
RS4-11	EC₅₀	0.014 μM Compound: Navitoclax, ABT-263	Induction of apoptosis in human RS4:11 cells overexpressing BCL-2 assessed as caspase 3/7 activation after 6 hrs by quantitative luminescence assay Induction of apoptosis in human RS4:11 cells overexpressing BCL-2 assessed as caspase 3/7 activation after 6 hrs by quantitative luminescence assay	[PMID: 24881567]
RS4-11	EC₅₀	0.11 μM Compound: 1; ABT-263	Cytotoxicity against human RS4-11 cells assessed as reduction in cell viability measured after 48 hrs by celltiter-glo assay Cytotoxicity against human RS4-11 cells assessed as reduction in cell viability measured after 48 hrs by celltiter-glo assay	[PMID: 34141086]
RS4-11	IC₅₀	42.6 nM Compound: ABT-263	Cytotoxicity against human RS4-11 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay Cytotoxicity against human RS4-11 cells assessed as reduction in cell viability measured after 48 hrs by MTS assay	[PMID: 34533954]
WI-38	IC₅₀	8.06 μM Compound: ABT-263	Cytotoxicity against human WI-38 cells assessed as cell viability measured after 72 hrs by MTS assay Cytotoxicity against human WI-38 cells assessed as cell viability measured after 72 hrs by MTS assay	[PMID: 32388279]

体外研究
(In Vitro)

Navitoclax (ABT-263) 对大约一半的 PPTP 体外面板细胞系具有活性。面板中所有线条的 IC₅₀ 中位数为 1.91 μM^[1]。Navitoclax 与化疗药物联用可使大多数卵巢癌细胞系产生协同反应，并增强 SK-OV-3 和 IGROV-1 细胞系中的半胱天冬酶活化^[2]。

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

体内研究
(In Vivo)

Navitoclax (100 mg/kg；口服；21 天处理) 增强 OSI-744 在体内的活性。作为单一药物，每天单独给予 100 mg/kg Navitoclax 没有显著的抗肿瘤活性，而每天给予 50 mg/kg 的 OSI-744 会在 21 天的处理期间导致显著的肿瘤停滞 (%TGI=52)。值得注意的是，Navitoclax 和 OSI-744 的组合连续 21 天每天服用可使 100% 接受处理的荷瘤小鼠产生 98% 的 TGI 和持久的肿瘤消退^[3]。

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

Animal Model:	Mice with NCI-H1650 model^[3]
Dosage:	100 mg/kg
Administration:	Orally; daily; for 21 consecutive days
Result:	As a single agent, 100 mg/kg alone dosed daily had no significant antitumor activity. Notably, the combination with OSI-744 resulted in 98% TGI and durable tumor regressions in 100% of treated tumor-bearing mice.

Clinical Trial

分子量

974.61

Formula

C₄₇H₅₅ClF₃N₅O₆S₃

CAS 号

923564-51-6

性状

固体

颜色

White to light yellow

中文名称

生根粉263

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	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMF 中的溶解度 : ≥ 100 mg/mL (102.61 mM)

DMSO 中的溶解度 : 75 mg/mL (76.95 mM; 超声助溶; 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	1.0261 mL	5.1303 mL	10.2605 mL
5 mM	0.2052 mL	1.0261 mL	2.0521 mL
10 mM	0.1026 mL	0.5130 mL	1.0261 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

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% Ethanol 60% Phosal 50 PG 30% PEG400
Solubility: 7.5 mg/mL (7.70 mM); 澄清溶液; 超声助溶
方案二

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (2.13 mM); 悬浊液; 超声助溶

此方案可获得 2.08 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 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。
方案三

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (2.13 mM); 悬浊液; 超声助溶

此方案可获得 2.08 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 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。
方案四

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (2.13 mM); 澄清溶液

此方案可获得 ≥ 2.08 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 20.8 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: 99.97% ee.: 99.92%

选择批次：

Data Sheet (645 KB) SDS (393 KB)

COA (290 KB) HNMR (233 KB) LCMS (122 KB) 元素分析报告 (212 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Lock R1, et al. Initial testing (stage 1) of the BH3 mimetic ABT-263 by the pediatric preclinical testing program. Pediatr Blood Cancer. 2008 Jun;50(6):1181-1189. [Content Brief]

[2]. Wong M, et al. Navitoclax (ABT-263) reduces Bcl-x(L)-mediated chemoresistance in ovarian cancer models.Mol Cancer Ther. 2012 Apr;11(4):1026-1035. [Content Brief]

[3]. Chen J, et al. The Bcl-2/Bcl-X(L)/Bcl-w inhibitor, navitoclax, enhances the activity of chemotherapeutic agents in vitro and in vivo. Mol Cancer Ther. 2011 Dec;10(12):2340-9. [Content Brief]

Navitoclax 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 / DMF	1 mM	1.0261 mL	5.1303 mL	10.2605 mL	25.6513 mL
	5 mM	0.2052 mL	1.0261 mL	2.0521 mL	5.1303 mL
	10 mM	0.1026 mL	0.5130 mL	1.0261 mL	2.5651 mL
	15 mM	0.0684 mL	0.3420 mL	0.6840 mL	1.7101 mL
	20 mM	0.0513 mL	0.2565 mL	0.5130 mL	1.2826 mL
	25 mM	0.0410 mL	0.2052 mL	0.4104 mL	1.0261 mL
	30 mM	0.0342 mL	0.1710 mL	0.3420 mL	0.8550 mL
	40 mM	0.0257 mL	0.1283 mL	0.2565 mL	0.6413 mL
	50 mM	0.0205 mL	0.1026 mL	0.2052 mL	0.5130 mL
	60 mM	0.0171 mL	0.0855 mL	0.1710 mL	0.4275 mL
DMF	80 mM	0.0128 mL	0.0641 mL	0.1283 mL	0.3206 mL
DMF	100 mM	0.0103 mL	0.0513 mL	0.1026 mL	0.2565 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:

Navitoclax923564-51-6ABT-263生根粉263ABT263ABT 263Bcl-2 FamilyInhibitorinhibitorinhibit

产品名称：			* 需求量：
* 客户姓名：			* Email：
* 电话：			* 公司或机构名称：
留言给我们：

产品名称：			* Lot #：
* 客户姓名：			* Email：
电话：			* 部门：
* 公司或机构名称：
留言给我们：

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）
Copyright © 2013-2025 MedChemExpress. All Rights Reserved.

Navitoclax (Synonyms: ABT-263)

Customer Review

Other Forms of Navitoclax:

MCE 顾客使用本产品发表的 92 篇科研文献

Navitoclax 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Bcl-2 Family 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

Navitoclax 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

姓名
邮箱 *

Sorry, but the email address you supplied was invalid.

Navitoclax (Synonyms: ABT-263)

Customer Review

Other Forms of Navitoclax:

Navitoclax 相关抗体

MCE 顾客使用本产品发表的 92 篇科研文献

Navitoclax 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Bcl-2 Family 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

Navitoclax 相关抗体:

摩尔计算器

稀释计算器

Navitoclax 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

Request for HNMR Report

Request for HNMR Report

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z