Idasanutlin (Synonyms: RG7388)

Name: Idasanutlin
Brand: MedChemExpress
SKU: HY-15676
Rating: 5.0 (38 reviews)

製品番号: HY-15676 純度: 99.93%: FAQs
Data Sheet SDS COA 取扱説明書

Molarity Calculator

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

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

Idasanutlin 構造式

CAS 番号 : 1229705-06-9

容量	価格（税別）	在庫状況	数量

無料サンプル (0.1 - 0.5 mg)		今すぐ申し込む
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 95	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 95	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	USD 70	在庫あり	Estimated Time of Arrival: December 31
10 mg	USD 120	在庫あり	Estimated Time of Arrival: December 31
50 mg	USD 290	在庫あり	Estimated Time of Arrival: December 31
100 mg	USD 490	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 38 publication(s) in Google Scholar

Other Forms of Idasanutlin:

Idasanutlin-d₃-1 在庫あり
Idasanutlin (enantiomer) 在庫あり

顧客検証

Cell Viability Assay

: Idasanutlin purchased from MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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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製品説明

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]

体外実験

Idasanutlin (RG7388) inhibits cell proliferation with IC₅₀ of 30 nM, and induces dose-dependent p53 stabilization, cell cycle arrest, as well as cell apoptosis in cancer cells expressing wild-type p53^[1].
Idasanutlin (RG7388) (300 nM or 1.8 μM) induces apoptosis in SJSA osteosarcoma cells^[2].

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

体内実験

Idasanutlin (RG7388, 25 mg/kg p.o.) results in tumor growth inhibition and regression, in the mouse SJSA human osteosarcoma xenograft model^[1].
Idasanutlin (RG7388) induces induction of apoptosis and antiproliferation, in the SJSA xenograft model^[2].

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

臨床実験

分子量

616.48

分子式

C₃₁H₂₉Cl₂F₂N₃O₄

CAS 番号

1229705-06-9

Appearance

Solid

Color

White to off-white

SMILES

O=C(O)C1=CC(OC)=C(NC([C@H]2[C@H](C3=C(F)C(Cl)=CC=C3)[C@](C4=CC=C(Cl)C=C4F)(C#N)[C@H](CC(C)(C)C)N2)=O)C=C1

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

溶剤 & 溶解度

体外:

DMSO : ≥ 45 mg/mL (73.00 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

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

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.06 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5%HPMC 1%Tween80
Solubility: 10 mg/mL (16.22 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 99.93%

Select Batch:

データシート (283 KB) SDS (0 KB)

COA (261 KB) RP-HPLC (244 KB) LCMS (93 KB) Elemental Analysis Report (119 KB)

取扱説明書 (2659 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]

細胞実験 ^[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. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[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. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

Idasanutlin Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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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Idasanutlin (Synonyms: RG7388)

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Other Forms of Idasanutlin:

Idasanutlin 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

生物活性

プロトコル

純度とドキュメンテーション

参考文献

カスタマーレビュー

Idasanutlin 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Idasanutlin Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

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