2. Cell Cycle/DNA Damage Epigenetics Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Stem Cell/Wnt JAK/STAT Signaling
  3. Aurora Kinase Bcr-Abl Akt STAT FLT3
  4. Cenisertib

Cenisertib  (Synonyms: AS-703569; R-763)

Cat. No.: HY-13072 Purity: 99.86%
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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.

For research use only. We do not sell to patients.

Cenisertib Chemical Structure

Cenisertib Chemical Structure

CAS No. : 871357-89-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 385 In-stock
Solution
10 mM * 1 mL in DMSO USD 385 In-stock
Solid
5 mg USD 350 In-stock
10 mg USD 550 In-stock
50 mg USD 1650 In-stock
100 mg USD 2250 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Cenisertib:

Cenisertib Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Cenisertib

View All Aurora Kinase Isoform Specific Products:

View All Isoforms
Aurora Kinase Aurora A Aurora B Aurora C

View All Akt Isoform Specific Products:

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Akt Akt1 Akt2 Akt3

View All STAT Isoform Specific Products:

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STAT3 STAT5 STAT6 STAT1

  • Biological Activity

  • Purity & Documentation

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Description

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[1][2][3].

IC50 & Target[1]

Aurora-A

 

Aurora-B

 

ABL1

 

STAT5

 

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.

Cenisertib Related Antibodies

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.
Clinical Trial
Molecular Weight

451.54

Formula

C24H30FN7O
CAS No.
Appearance

Solid

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]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2146 mL 11.0732 mL 22.1464 mL
5 mM 0.4429 mL 2.2146 mL 4.4293 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, 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.

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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    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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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.
Purity & Documentation
References

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, 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
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Cenisertib Related Classifications

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:

Cenisertib871357-89-0AS-703569 R-763AS703569AS 703569R763R 763R-763Aurora KinaseBcr-AblAktSTATFLT3PKBProtein kinase BCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Inhibitorinhibitorinhibit

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