Cenisertib

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].

Product Specifications

CAS Number

[871357-89-0]

Product Name Alternative

AS-703569; R-763

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

Akt; Aurora Kinase; Bcr-Abl; FLT3; STAT

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; JAK/STAT Signaling; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/cenisertib.html

Purity

99.86

Solubility

DMSO : 250 mg/mL (ultrasonic)

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]

Molecular Formula

C24H30FN7O

Molecular Weight

451.54

Precautions

H302, H315, H319

References & Citations

[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.|[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.|[3]Maryam Shariati, et al. Targeting AKT for cancer therapy. Expert Opin Investig Drugs. 2019 Nov;28 (11) :977-988.