2196186-84-0
Chemical Structure
APG-2449
- CAS No.: 2196186-84-0
- Formula:C33H42ClN5O4S
- Molecular Weight:640.24
InChIKey: YWPHBSHEGTZPNS-UHFFFAOYSA-N
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
Biological Activity: 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].
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APG-2449 | 98.93% | 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. | ||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
Keywords
