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

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

Cat. No.: HY-13072
Handling Instructions

Cenisertib (AS-703569) is a 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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Cenisertib Chemical Structure

Cenisertib Chemical Structure

CAS No. : 871357-89-0

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Description

Cenisertib (AS-703569) is a 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)[1]. Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia[2].

IC50 & Target[1]

Aurora-A

 

Aurora-B

 

ABL1

 

Akt

 

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].

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) significantly suppresses tumor growth.

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
Result: Suppressed significantly tumor growth.
Molecular Weight

451.54

Formula

C₂₄H₃₀FN₇O

CAS No.

871357-89-0

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]

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Room temperature in continental US; may vary elsewhere

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Please store the product under the recommended conditions in the Certificate of Analysis.

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