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APG-2449

CAT: 0804-HY-155163-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-155163-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1