製品番号: HY-16999

RO8994

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Based on 1 Customer Validation

RO8994 (Compound 4) is an orally active, highly potent and selective spiroindolinone p53-MDM2 inhibitor with an IC₅₀ value of 5 nM (HTRF binding assays) and 20 nM (MTT proliferation assays). RO8994 induces up-regulation of p53 expression and Apoptosis in wild-type p53 cancer cells. RO8994 also inhibits tumor growth in the tumor xenograft model.

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純度: 99.70%
CAS 番号: 1309684-94-3
分子式: C₃₁H₃₁Cl₂FN₄O₄
分子量:613.51

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

RO8994 構造式

CAS 番号: 1309684-94-3

容量

価格（税別）

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数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- Cellular Effect
- 体外実験
- 体内実験
化学情報
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

Cellular Effect

Cell Line	Type	Value	Description	References
SJSA-1	IC₅₀	0.013 μM Compound: RO8994	Antiproliferative activity against human SJSA cells expressing wild-type p53 by MTT assay Antiproliferative activity against human SJSA cells expressing wild-type p53 by MTT assay	[PMID: 24900784]
SW480	IC₅₀	5.19 μM Compound: RO8994	Antiproliferative activity against human SW480 cells expressing p53 mutant by MTT assay Antiproliferative activity against human SW480 cells expressing p53 mutant by MTT assay	[PMID: 24900784]

体外実験

RO8994 dose-dependently and non-genotoxically induces p53 stabilization, cell cycle arrest and Apoptosis in tumor cells retainingwt p53^[3].

Activity Results for RO8994 in a Biochemical Binding Assay and Human Cancer Cell Proliferation Assays^[1]^[2]^[3]<

compd	HTRF IC₅₀ (nM)	SJSA IC₅₀ (μM)	SW480 IC₅₀ (μM)
RO8994	5	0.013	5.19

Antiproliferative Activity of RO8994 in Human Cancer Cell lines^[1]^[2]^[3]<

compd	MTT IC₅₀ (μM)	selectivity
RO8994	0.02	312

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

体内実験

RO8994 inhibits tumor growth in human SJSA1 tumor xenografts models^[3].

Human Liver Microsomal Stability and Mean Single Dose PK Parameters of RO8994 in C57 Male Mice by Oral and IV Dosing^[1]^[2]^[3]<

compd	HLM_{_}CL (mL/min/kg)	PO dose (mg/kg)	PO AUC/dose (μg·hr/mL/mg/kg)	PO C_max (μg/mL)	IV dose (mg/kg)	CL (mL/min/kg)	t_1/2 (h)	F (%)
RO8994	7.5	25	3.7	5.8	0.64	5.8	7.1	92

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

化学情報

CAS 番号 1309684-94-3
性状 Solid
分子量 613.51
分子式 C₃₁H₃₁Cl₂FN₄O₄
Color White to off-white
SMILES

O=C([C@H](N[C@H]1CC(C)(C)C)[C@H](C2=CC=CC(Cl)=C2F)[C@@]31C(NC4=C3C=CC(Cl)=C4)=O)NC5=CC=C(C(N)=O)C=C5OC
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	2 years
	-20°C	1 year

溶剤 & 溶解度

体外:

DMSO : ≥ 45 mg/mL (73.35 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6300 mL

8.1498 mL

16.2997 mL

5 mM

0.3260 mL

1.6300 mL

3.2599 mL

10 mM

0.1630 mL

0.8150 mL

1.6300 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

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

Stock Solution Working Solution

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (3.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (281 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Zhang Z, et al. Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy. Bioorg Med Chem. 2014 Aug 1;22(15):4001-4009. [Content Brief]

[2]. Zhang Z, et al. Discovery of Potent and Orally Active p53-MDM2 Inhibitors RO5353 and RO2468 for Potential Clinical Development. ACS Med Chem Lett. 2013 Dec 29;5(2):124-7. [Content Brief]

[3]. Yu B, Liu H M. The development of new spirooxindoles targeting the p53–MDM2 protein-protein interactions for cancer therapy[J]. Targeting Protein-Protein Interactions by Small Molecules, 2018: 213-237.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.6300 mL	8.1498 mL	16.2997 mL	40.7491 mL
	5 mM	0.3260 mL	1.6300 mL	3.2599 mL	8.1498 mL
	10 mM	0.1630 mL	0.8150 mL	1.6300 mL	4.0749 mL
	15 mM	0.1087 mL	0.5433 mL	1.0866 mL	2.7166 mL
	20 mM	0.0815 mL	0.4075 mL	0.8150 mL	2.0375 mL
	25 mM	0.0652 mL	0.3260 mL	0.6520 mL	1.6300 mL
	30 mM	0.0543 mL	0.2717 mL	0.5433 mL	1.3583 mL
	40 mM	0.0407 mL	0.2037 mL	0.4075 mL	1.0187 mL
	50 mM	0.0326 mL	0.1630 mL	0.3260 mL	0.8150 mL
	60 mM	0.0272 mL	0.1358 mL	0.2717 mL	0.6792 mL

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RO8994

Oxygen Sensing Compound Library

Ubiquitination Compound Library

Ferroptosis Compound Library

Pyroptosis Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Amino Acid Metabolism Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Apoptosis Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

生物活性

化学情報

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

RO8994 関連分類

HY-16999 関連分類