APG-2449

APG-2449 is an orally active inhibitor for BCL-2 and multikinase (ALK/FAK/ROS1) with potent antitumor activities. APG-2449 reduces cell viability and enhances apoptosis in acute myeloid leukemia cells in vitro. APG-2449 decreases activation of FAK and its downstream effectors. APG-2449 can be studied in research for mesothelioma tumor, non-small cell lung cancer, ovarian cancer, hematologic and solid malignancies[1][2][3][4].

Product Specifications

CAS Number

[2196186-84-0]

UNSPSC

12352005

Target

Anaplastic lymphoma kinase (ALK) ; Apoptosis; FAK; ROS Kinase

Type

Reference compound

Related Pathways

Apoptosis; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/apg-2449.html

Purity

98.93

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

O=S(C1=C(NC2=NC(NC3=CC(C)=C(C4=CCN(C5CCOCC5)CC4)C=C3OC(C)C)=NC=C2Cl)C=CC=C1)(C(C)C)=O

Molecular Formula

C33H42ClN5O4S

Molecular Weight

640.24

References & Citations

[1]Fang DD, et al. Discovery of a novel ALK/ROS1/FAK inhibitor, APG-2449, in preclinical non-small cell lung cancer and ovarian cancer models. BMC Cancer. 2022 Jul 11;22 (1) :752.|[2]Ran Tao, et al., Abstract 2563: FAK inhibitor APG-2449 and CDK4/6 inhibitor palbociclib synergistically suppress mesothelioma tumor growth via autophagy induction. Cancer Res 15 June 2022; 82 (12_Supplement) : 2563. |[3]Zhou Yu, et al., APG-2449, a Novel Focal Adhesion Kinase (FAK) Inhibitor, Exhibits Antileukemic Activity and Enhances Lisaftoclax (APG-2575) -Induced Apoptosis in Acute Myeloid Leukemia (AML) . Blood 2024; 144 (Supplement 1) : 4150.|[4]Luo, Q. Y., et al., (2021) . A multi-kinase inhibitor APG-2449 enhances the antitumor effect of ibrutinib in esophageal squamous cell carcinoma via EGFR/FAK pathway inhibition. Biochemical pharmacology, 183, 114318.