Cat. No.: HY-13072

Cenisertib

(Synonyms: AS-703569; R-763)

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Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia.

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Pureté: 99.86%
CAS No.: 871357-89-0
Formule: C₂₄H₃₀FN₇O
Masse moléculaire:451.54

Stockage:

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

Cenisertib Chemical Structure

CAS No.: 871357-89-0

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Fluorescent Dye

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

Aurora-A

Aurora-B

ABL1

STAT5

Voir tous les produits spécifiques à Isoform Aurora Kinase :

Voir tous les produits spécifiques à Isoform Bcr-Abl :

Abl
Bcr-Abl

Voir tous les produits spécifiques à Isoform Akt :

Voir tous les produits spécifiques à Isoform STAT :

Cellular Effect

Cell Line	Type	Value	Description	References
NIH3T3	IC₅₀	19 nM Compound: (+)-2 (AS 703569)	Inhibition of human KDR autophosphorylation expressed in mouse NIH/3T3 cells Inhibition of human KDR autophosphorylation expressed in mouse NIH/3T3 cells	[PMID: 22695126]

In Vitro

Cenisertib (AS-703569) (1-1000 nM; for 48 hours) induces dose-dependent inhibition of proliferation in primary neoplastic mast cells (MC) ^[1].
Cenisertib (5-100 nM; for 24 hours) induces a substantial G2/M cell cycle arrest at low nanomolar concentrations in all MC lines^[1].
Cenisertib (1-1000 nM; for 24 hours)induces apoptosis in HMC-1.1, HMC-1.2, C2, and NI-1 cells in a dose-dependent manner^[1].
Cenisertib (5-500 nM; for 24 hours) induces cleavage of caspase 3 in both HMC-1 sub-clones as well as in C2 and NI-1 cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

HMC-1.1, HMC-1.2, ROSAKIT WT, ROSAKIT D816V and MCPV-1.1 mast cells
Concentration:

1, 5, 10, 50, 100, 500, 1000 nM
Incubation Time:

48 hours
Result:

Induced dose-dependent inhibition of proliferation in primary neoplastic MC.

Cell Cycle Analysis^[1]

Cell Line:

HMC-1.1, HMC-1.2, C2 and NI-1 cells
Concentration:

5, 10, 50, 100 nM
Incubation Time:

24 hours
Result:

Induced a substantial G2/M cell cycle arrest at low nanomolar concentrations in all MC lines.

Apoptosis Analysis^[1]

Cell Line:

HMC-1.1, HMC-1.2, C2 and NI-1 cells
Concentration:

1, 5, 10, 50, 100, 500, 1000 nM
Incubation Time:

24 hours
Result:

Induced apoptosis in HMC-1.1, HMC-1.2, C2, and NI-1 cells in a dose-dependent manner.

Western Blot Analysis^[1]

Cell Line:

HMC-1.1, HMC-1.2, C2 and NI-1 cells
Concentration:

50, 100, 500 nM
Incubation Time:

24 hours
Result:

Induced cleavage of caspase 3 in both HMC-1 sub-clones as well as in C2 and NI-1 cells.

In Vivo

Cenisertib (AS-703569) (orally; 7 or 10 mg/kg/day; for 3 days followed by a 4-day rest period; for 4 weeks) significantly suppresses tumor growth.

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

Animal Model:

Female CB17 Severe Combined Immunodeficiency (SCID) mice bearing NCI-MDR tumors^[2]
Dosage:

7 and 10 mg/kg
Administration:

Orally; daily; for 3 days followed by a 4-day rest period; for 4 weeks
Result:

Suppressed significantly tumor growth.

Essai clinique

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

Chemical Information

CAS No. 871357-89-0
Appearance Solid
Masse moléculaire 451.54
Formule C₂₄H₃₀FN₇O
Color White to off-white
SMILES

[H][C@@]1([C@H]([C@H]2C(N)=O)NC3=NC(NC4=CC=C(C(C)=C4)N5CCN(CC5)C)=NC=C3F)C[C@]2(C=C1)[H]
Synonyms

AS-703569; R-763
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (1)

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Patent

US20210299273A1.

Solvant et solubilité

In Vitro:

DMSO : 250 mg/mL (553.66 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

2.2146 mL

11.0732 mL

22.1464 mL

5 mM

0.4429 mL

2.2146 mL

4.4293 mL

10 mM

0.2215 mL

1.1073 mL

2.2146 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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 (4.61 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% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (4.61 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.08 mg/mL (4.61 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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (282 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)
Elemental Analysis Report (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)
Instruction de manipulation (2659 KB)

Références

[1]. Peter B, et al. Drug-induced inhibition of phosphorylation of STAT5 overrides drug resistance in neoplastic mast cells. Leukemia. 2018 Apr;32(4):1016-1022. [Content Brief]

[2]. McLaughlin J, et al. Preclinical characterization of Aurora kinase inhibitor R763/AS703569 identified through an image-based phenotypic screen. J Cancer Res Clin Oncol. 2010 Jan;136(1):99-113. [Content Brief]

[3]. Maryam Shariati, et al. Targeting AKT for cancer therapy. Expert Opin Investig Drugs. 2019 Nov;28(11):977-988. [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	2.2146 mL	11.0732 mL	22.1464 mL	55.3661 mL
	5 mM	0.4429 mL	2.2146 mL	4.4293 mL	11.0732 mL
	10 mM	0.2215 mL	1.1073 mL	2.2146 mL	5.5366 mL
	15 mM	0.1476 mL	0.7382 mL	1.4764 mL	3.6911 mL
	20 mM	0.1107 mL	0.5537 mL	1.1073 mL	2.7683 mL
	25 mM	0.0886 mL	0.4429 mL	0.8859 mL	2.2146 mL
	30 mM	0.0738 mL	0.3691 mL	0.7382 mL	1.8455 mL
	40 mM	0.0554 mL	0.2768 mL	0.5537 mL	1.3842 mL
	50 mM	0.0443 mL	0.2215 mL	0.4429 mL	1.1073 mL
	60 mM	0.0369 mL	0.1846 mL	0.3691 mL	0.9228 mL
	80 mM	0.0277 mL	0.1384 mL	0.2768 mL	0.6921 mL
	100 mM	0.0221 mL	0.1107 mL	0.2215 mL	0.5537 mL

Keywords

Cenisertib

1 Cited Publications

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Cenisertib

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Publications Citing Use of MedChemExpress (MCE) Cenisertib

Voir tous les produits spécifiques à Isoform Aurora Kinase

Voir tous les produits spécifiques à Isoform Bcr-Abl

Voir tous les produits spécifiques à Isoform Akt

Voir tous les produits spécifiques à Isoform STAT

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Cenisertib Related Classifications

HY-13072 Related Classifications