Idasanutlin (Synonyms: RG7388)

目录号: HY-15676 纯度: 99.93%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Idasanutlin (RG7388) 是一种有效，选择性的 MDM2 拮抗剂，能够抑制 p53-MDM2 的结合，IC₅₀ 值为 6 nM。

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Idasanutlin Chemical Structure

CAS No. : 1229705-06-9

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1221	In-stock
5 mg	￥900	In-stock
10 mg	￥1350	In-stock
50 mg	￥3950	In-stock
100 mg	￥5950	In-stock
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Idasanutlin:

MCE 顾客使用本产品发表的 37 篇科研文献

Cell Viability Assay

: Idasanutlin purchased from MCE. Usage Cited in: Nat Commun. 2023 Apr 6;14(1):1941. [Abstract]; Idasanutlin (RG7388; 1, 2.5, 10 μM; 30 min) reverses the Mdm2-induced decreased expression of p53 in H1299 cells.

: Idasanutlin purchased from MCE. Usage Cited in: Sci Pharm. 2023 Feb;91(1), 12.; Idasanutlin (1, 10, 30 µM; 24 h) inhibits viability of MCF-7 cells.

: Idasanutlin purchased from MCE. Usage Cited in: Cancer Res. 2019 May 1;79(9):2404-2414. [Abstract]; Immunoblot for p53 pathway responses to 壹dasanutlin treatment (1 μM for 24h) in TTC642 cells reexpressing SMARCB1. Images are representative of three biological replicates.

: Idasanutlin purchased from MCE. Usage Cited in: Cells. 2018 Dec 22;8(1). pii: E8. [Abstract]; Modulation of necroptosis-related protein expressions in MCF-7 cells after (7.5 μM), RG7388 (2.0 μM) and SAHA + RG7388 treatment for 24 h

: Idasanutlin purchased from MCE. Usage Cited in: Cells. 2018 Dec 22;8(1). pii: E8. [Abstract]; Modulation of apoptosis-related protein expressions in MCF-7 cells after SAHA (7.5 μM), RG7388 (2.0 μM) and SAHA + RG7388 treatment for 24 h.

: Idasanutlin purchased from MCE. Usage Cited in: Medicina (Kaunas). 2019 Jan 29;55(2):30. [Abstract]; Effect of SAHA and RG7388 treatments on Cell Cycle related Protein levels in MCF-7 cells. Figure shows upregulation of p21, p27, AURKB and CDC25C levels after treatment with 7.5 µM concentration of SAHA and p53 upregulation after RG7388 treatment.

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Idasanutlin (RG7388) is a potent and selective MDM2 antagonist, inhibiting p53-MDM2 binding, with an IC₅₀ of 6 nM.

IC₅₀ & Target

IC50: 6 nM (p53-MDM2)^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	0.01 μM Compound: 12, RG7388	Cytotoxicity against human HCT116 cells expressing wild type p53 assessed as growth inhibition by MTT assay Cytotoxicity against human HCT116 cells expressing wild type p53 assessed as growth inhibition by MTT assay	[PMID: 23808545]
MDA-MB-435	IC₅₀	9.1 μM Compound: 12, RG7388	Cytotoxicity against human MDA-MB-435 cells expressing p53 mutant assessed as growth inhibition by MTT assay Cytotoxicity against human MDA-MB-435 cells expressing p53 mutant assessed as growth inhibition by MTT assay	[PMID: 23808545]
RKO	IC₅₀	0.07 μM Compound: 12, RG7388	Cytotoxicity against human RKO cells expressing wild type p53 assessed as growth inhibition by MTT assay Cytotoxicity against human RKO cells expressing wild type p53 assessed as growth inhibition by MTT assay	[PMID: 23808545]
SJSA-1	IC₅₀	0.01 μM Compound: 12, RG7388	Cytotoxicity against human SJSA1 cells expressing wild type p53 assessed as growth inhibition by MTT assay Cytotoxicity against human SJSA1 cells expressing wild type p53 assessed as growth inhibition by MTT assay	[PMID: 23808545]
SJSA-1	IC₅₀	45 nM Compound: RG7388	Antiproliferative activity against human SJSA1 cells assessed as inhibition of EdU incorporation after 1 hr by Click-iT EdU HCS assay in presence of 10% human serum Antiproliferative activity against human SJSA1 cells assessed as inhibition of EdU incorporation after 1 hr by Click-iT EdU HCS assay in presence of 10% human serum	[PMID: 24456472]
SJSA-1	IC₅₀	45 nM Compound: RG7388	Cytotoxicity against human SJSA1 cells assessed as growth inhibition after 16 hrs by EdU incorporation assay in presence of 10% human serum Cytotoxicity against human SJSA1 cells assessed as growth inhibition after 16 hrs by EdU incorporation assay in presence of 10% human serum	[PMID: 24601644]
SW480	IC₅₀	13.3 μM Compound: 12, RG7388	Cytotoxicity against human SW480 cells expressing p53 mutant assessed as growth inhibition by MTT assay Cytotoxicity against human SW480 cells expressing p53 mutant assessed as growth inhibition by MTT assay	[PMID: 23808545]

体外研究
(In Vitro)

Idasanutlin (RG7388) 抑制细胞增殖，IC₅₀ 为 30 nM，并在表达野生型 p53 的癌细胞中诱导剂量依赖性 p53 稳定、细胞周期停滞以及细胞凋亡^[1]。
Idasanutlin (RG7388) (300 nM 或 1.8 μM) 诱导 SJSA 骨肉瘤细胞凋亡^[2]。

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

体内研究
(In Vivo)

Idasanutlin (RG7388，25 mg/kg po) 在小鼠 SJSA 人骨肉瘤异种移植模型中导致肿瘤生长抑制和消退^[1]。
Idasanutlin (RG7388) 在 SJSA 异种移植模型中诱导细胞凋亡和抗增殖^[2]。

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

Clinical Trial

分子量

616.48

Formula

C₃₁H₂₉Cl₂F₂N₃O₄

CAS 号

1229705-06-9

性状

固体

颜色

White to off-white

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 : ≥ 45 mg/mL (73.00 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	1.6221 mL	8.1106 mL	16.2211 mL
5 mM	0.3244 mL	1.6221 mL	3.2442 mL
10 mM	0.1622 mL	0.8111 mL	1.6221 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 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.06 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。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。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： 0.5% HPMC/1% Tween-80 in Saline water
Solubility: 10 mg/mL (16.22 mM); 悬浊液; 超声助溶

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: 99.93%

选择批次：

Data Sheet (639 KB) SDS (393 KB)

COA (299 KB) RP-HPLC (244 KB) LCMS (93 KB) 元素分析报告 (222 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Ding Q, et al. Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. J Med Chem. 2013 Jul 25;56(14):5979-83. [Content Brief]

[2]. Higgins B, et al. Preclinical optimization of MDM2 antagonist scheduling for cancer treatment by using a model-based approach. Clin Cancer Res. 2014, 20(14), 3742-3752. [Content Brief]

Cell Assay ^[1]	Cell proliferation is evaluated by the tetrazolium dye assay. The concentration at which 50% inhibition (IC₅₀) or 90% inhibition (IC₉₀) of cell proliferation is determined from the linear regression of a plot of the logarithm of the concentration versus percent inhibition. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	At 10 to 12 weeks of age, mice are implanted with a 1:1 mixture of human SJSA osteosarcoma cells (ATCC) suspended in phenol-free Matrigel and PBS. Mice are implanted in the right flank at a concentration of 5×10⁶ cells in 0.2 mL total volume. At approximately day 10, animals are randomized according to tumor volume, so that all groups of 10 randomized mice have similar starting mean tumor volumes of 100 to 250 mm³. Idasanutlin (RG7388) is administered as an amorphous solid dispersion microbulk precipitate powder containing 30% drug substance and 70% hydroxypropyl methylcellulose acetate succinate polymer that is reconstituted immediately before administration as a suspension in Klucel/Tween, and remaining suspension is discarded after dosing. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Ding Q, et al. Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development. J Med Chem. 2013 Jul 25;56(14):5979-83. [Content Brief] [2]. Higgins B, et al. Preclinical optimization of MDM2 antagonist scheduling for cancer treatment by using a model-based approach. Clin Cancer Res. 2014, 20(14), 3742-3752. [Content Brief]

Idasanutlin 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	1.6221 mL	8.1106 mL	16.2211 mL	40.5528 mL
	5 mM	0.3244 mL	1.6221 mL	3.2442 mL	8.1106 mL
	10 mM	0.1622 mL	0.8111 mL	1.6221 mL	4.0553 mL
	15 mM	0.1081 mL	0.5407 mL	1.0814 mL	2.7035 mL
	20 mM	0.0811 mL	0.4055 mL	0.8111 mL	2.0276 mL
	25 mM	0.0649 mL	0.3244 mL	0.6488 mL	1.6221 mL
	30 mM	0.0541 mL	0.2704 mL	0.5407 mL	1.3518 mL
	40 mM	0.0406 mL	0.2028 mL	0.4055 mL	1.0138 mL
	50 mM	0.0324 mL	0.1622 mL	0.3244 mL	0.8111 mL
	60 mM	0.0270 mL	0.1352 mL	0.2704 mL	0.6759 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:

Idasanutlin1229705-06-9RG7388RG 7388RG-7388MDM-2/p53E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseInhibitorinhibitorinhibit

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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）

Idasanutlin (Synonyms: RG7388)

Customer Review

Other Forms of Idasanutlin:

MCE 顾客使用本产品发表的 37 篇科研文献