製品番号: HY-16956

Onatasertib

(別名: CC-223; ATG-008)

3 Cited Publications

カスタマーレビュー

Based on 3 publication(s) in Google Scholar

Onatasertib (CC-223) is a potent, selective, and orally bioavailable inhibitor of mTOR kinase, with an IC₅₀ value for mTOR kinase of 16 nM. Onatasertib inhibits both mTORC1 and mTORC2.

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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。

純度: 99.47%
CAS 番号: 1228013-30-6
分子式: C₂₁H₂₇N₅O₃
分子量:397.47

保管条件:

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

Onatasertib 構造式

CAS 番号: 1228013-30-6

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数量

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Fluorescent Dye

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (3)
溶剤 & 溶解度
- 体外
- 体内
プロトコル
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

IC₅₀ & Target^[1]

mTOR

16 nM (IC₅₀)

mTORC1

mTORC2

DNA-PK

0.84 μM (IC₅₀)

PI3K-α

4 μM (IC₅₀)

mTOR アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
Caco-2	CC₅₀	9.49 μM Compound: CC-223	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay	10.21203/rs.3.rs-23951/v1
Caco-2	IC₅₀	16.78 μM Compound: CC-223	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging	10.21203/rs.3.rs-23951/v1
PC-3	IC₅₀	0.01 μM Compound: 37, CC-223	Inhibition of mTORC2 in human PC3 cells assessed as inhibition of Akt phosphorylation at S473 after 1 hr Inhibition of mTORC2 in human PC3 cells assessed as inhibition of Akt phosphorylation at S473 after 1 hr	[PMID: 26083478]
PC-3	IC₅₀	0.03 μM Compound: 37, CC-223	Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr Inhibition of mTORC1 in human PC3 cells assessed as inhibition of S6 phosphorylation after 1 hr	[PMID: 26083478]

体外実験

Onatasertib is a potent, selective, and orally bioavailable inhibitor of mTOR kinase, demonstrating inhibition of mTORC1 (pS6RP and p4EBP1) and mTORC2 [pAKT(S473)] in cellular systems. Onatasertib is selective for mTOR kinase with >200-fold selectivity over the related PI3K-α (IC₅₀=4.0 μM). Of the PI3K related kinases tested, Onatasertib shows no significant inhibition of ATR or SMG1 and inhibits DNA-PK with an IC₅₀ value of 0.84 μM. When screened in a single-point assay against a commercially available panel of 246 kinases, only three kinases other than mTOR are inhibited >80% at 10 μM by Onatasertib. Upon follow-up IC₅₀ value determination, only two are inhibited by Onatasertib with IC₅₀ values below 1 μM; FLT4 (0.651 μM) and cFMS (0.028 μM). The exquisite kinase selectivity of Onatasertib is confirmed upon evaluation in cellular systems using ActivX KiNavtiv profiling. Other than mTOR kinase, no kinase target is identified when HCT 116 or A549 cells are treated for 1 hour with 1 μM Onatasertib and assayed for kinase activity. Onatasertib shows a concentration-dependent reduction in each marker, with IC₅₀ values of 31±2 nM for pS6RP, 405±47 nM for p4EBP1, and 11±10 nM for pAKT(S473) in western blot analysis. Inhibition of these pathway biomarkers is investigated in additional cell types from a variety of tissue origins. Onatasertib inhibits both mTORC1 (S6RP and 4EBP1) and mTORC2 [AKT(S473)] markers across the panel with IC₅₀ ranges of 27 to 184 nM for pS6RP, 120 to 1,050 nM for p4EBP1 and 11 to 150 nM for pAKT(S473) ^[1].

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

体内実験

The antitumor activity of Onatasertib in the PC-3 xenograft model is determined using a number of dosing paradigms. Onatasertib significantly inhibits PC-3 tumor growth in a dose- and schedule-dependent manner. Dosing at 10 or 25 mg/kg, once daily, results in 46% (P<0.001) and 87% (P<0.001) reduction in tumor volume, respectively. Similar dose dependency is observed with twice-daily dosing at 5 or 10 mg/kg, corresponding to 65% (P<0.001) and 80% (P<0.001) tumor volume reductions. All dose levels are tolerated in the once-daily and twice-daily dosing studies, with only the 25 mg/kg/d group showing any significant body weight loss. These mice lost approximately 10% of their initial body weight after 3 weeks of dosing^[1].

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

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 1228013-30-6
性状 Solid
分子量 397.47
分子式 C₂₁H₂₇N₅O₃
Color Light yellow to yellow
SMILES

O=C1CNC2=NC=C(C3=CC=C(C(C)(O)C)N=C3)N=C2N1[C@H]4CC[C@H](OC)CC4
別名

CC-223; ATG-008
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

Publications (3)

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Front Pharmacol

CC-223, NSC781406, and BGT226 Exerts a Cytotoxic Effect Against Pancreatic Cancer Cells via mTOR Signaling. [Abstract]

2020 Nov 11;11:580407. PMID: 33343350
bioRxiv

2025 Aug 31.
Oncotarget

Preclinical study of CC223 as a potential anti-ovarian cancer agent. [Abstract]

2017 May 10;8(35):58469-58479. PMID: 28938571

Onatasertib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 May 10;8(35):58469-58479. [Abstract]

CC223 blocks mTORC1 and mTORC2 activation in SKOV3 cells. SKOV3 cells are treated with CC223 (100 nM), cells are further cultured for implied time, mTOR-Raptor and mTOR-Rictor assembly is tested by Co-immunoprecipitation assay. Expressions of listed proteins are tested by the Western blotting assay.

溶剤 & 溶解度

体外:

DMSO : 50 mg/mL (125.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.5159 mL

12.5796 mL

25.1591 mL

5 mM

0.5032 mL

2.5159 mL

5.0318 mL

10 mM

0.2516 mL

1.2580 mL

2.5159 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: ≥ 1.25 mg/mL (3.14 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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% (20% SBE-β-CD in Saline)

Solubility: ≥ 1.25 mg/mL (3.14 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, 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

プロトコル

Kinase Assay^[1]

Counter screen against 246 protein kinases is outsourced and completed at a fixed CC-223 concentration (10 μM). Follow-up IC₅₀ value determinations for ephrin type-B receptor 3 kinase (EPHB3), colony stimulating factor 1 receptor tyrosine kinase (CSF1R or cFMS), and FMS-related tyrosine kinase 4 (FLT4) are outsourced to Invitrogen^[1].

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

Cell Assay^[1]

For other cell panel proliferation assays, CC-223 (1 nM, 100 nM and 1 μM) is spotted via an acoustic dispenser (EDC ATS-100) into an empty 384-well plate. Cells are diluted to desired densities and added directly to the compound-spotted plates. Cells are allowed to grow for 72 hours. Viability is assessed via Cell Titer-Glo. All data are normalized and represented as a percentage of the DMSO-treated cells. Results are then expressed as GI₅₀ and/or IC₅₀ values^[1].

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

Animal Administration^[1]

Mice^[1]
Female 6- to 8-weeks-old CB17 SCID mice are inoculated s.c. with 2×10⁶ PC-3 cells. When tumors reach approximately 125 mm³, mice are randomized and treated once daily, twice daily, or every 2 days orally with vehicle or various doses of CC-223, at a dose volume of 5 mL/kg. The twice-daily doses are administered with a 10 hours separation between the morning and evening doses. Tumor volumes are determined before the initiation of treatment and are considered as the starting volumes. Tumors are measured twice a week for the duration of the study. The long and short axes of each tumor are measured using a digital caliper in millimeters. The tumor volumes are calculated. The tumor volumes are expressed in cubic millimeters (mm³).

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

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 (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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]. Mortensen DS, et al. CC-223, a Potent and Selective Inhibitor of mTOR Kinase: In Vitro and In Vivo Characterization. Mol Cancer Ther. 2015 Jun;14(6):1295-305. [Content Brief]

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	2.5159 mL	12.5796 mL	25.1591 mL	62.8978 mL
	5 mM	0.5032 mL	2.5159 mL	5.0318 mL	12.5796 mL
	10 mM	0.2516 mL	1.2580 mL	2.5159 mL	6.2898 mL
	15 mM	0.1677 mL	0.8386 mL	1.6773 mL	4.1932 mL
	20 mM	0.1258 mL	0.6290 mL	1.2580 mL	3.1449 mL
	25 mM	0.1006 mL	0.5032 mL	1.0064 mL	2.5159 mL
	30 mM	0.0839 mL	0.4193 mL	0.8386 mL	2.0966 mL
	40 mM	0.0629 mL	0.3145 mL	0.6290 mL	1.5724 mL
	50 mM	0.0503 mL	0.2516 mL	0.5032 mL	1.2580 mL
	60 mM	0.0419 mL	0.2097 mL	0.4193 mL	1.0483 mL
	80 mM	0.0314 mL	0.1572 mL	0.3145 mL	0.7862 mL
	100 mM	0.0252 mL	0.1258 mL	0.2516 mL	0.6290 mL

Keywords

Onatasertib

3 Cited Publications

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Onatasertib

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MedChemExpress（MCE）の使用を引用している文献 Onatasertib

mTOR アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (3)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Onatasertib 関連分類

HY-16956 関連分類