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: 99.64%
COA Handling Instructions

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

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Solution
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 385 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Cenisertib

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Aurora Kinase Aurora A Aurora B Aurora C

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Akt Akt1 Akt2 Akt3

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STAT3 STAT5 STAT6 STAT1

  • Biological Activity

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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].

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.

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

Appearance

Solid

Formula

C24H30FN7O
CAS No.
SMILES

[H][[email protected]@]1([[email protected]]([[email protected]]2C(N)=O)NC3=NC(NC4=CC=C(C(C)=C4)N5CCN(CC5)C)=NC=C3F)C[[email protected]]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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (553.66 mM; Need ultrasonic)

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
10 mM 0.2215 mL 1.1073 mL 2.2146 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.61 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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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.

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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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