Art. -Nr.: HY-155163

APG-2449

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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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Reinheit: 98.93%
CAS. Nr.: 2196186-84-0
Formel: C₃₃H₄₂ClN₅O₄S
Molecular Weight:640.24

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

APG-2449 Chemical Structure

CAS. Nr.: 2196186-84-0

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

APG-2449 inhibits ALK, ROS1, and FAK with Kd values if 1.6, 0.81, and 5.4 nM, respectively^[1].
APG-2449 exhibits moderate antiproliferative activity in cells without ALK or ROS1 rearrangements but with detectable expression of FAK protein (e.g. IC₅₀ = 3.55 μM in NCI-H1975 and 2.71 μM in PA-1)^[1].
APG-2449 (0-10 μM, 6-24 h) exerts anti-cancer effect mediated by suppressing ALK- or ROS1-driven signaling pathway in HCC78 cells carrying SLC34A2-ROS1 fusion^[1].
APG-2449 (0-10 μM, 4 h) downregulates p-FAK and downstream signaling factors in PA-1 ovarian cancer cells^[1].
APG-2449 (1-5 μM, 72 h) dose-dependently decreases numbers of CD44⁺ and ALDH1⁺ SKOV-3 ovarian cancer stem cells^[1].
APG-2449 (0.5-1 μM, 14 d) significantly decreases the colony formation in KYSE-150 and KYSE-520 cells^[4].
APG-2449 (1-2 μM, 24 h) inhibits the migration ability of esophageal squamous cell carcinoma (ESCC) cells^[4].
APG-2449 (0-2 μM, 24-72 h) significantly suppresses cell viability when combined with Ibrutinib (HY-10997) compared with single-agent in KYSE-150 and KYSE-520 cells^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

HCC78 cells carrying SLC34A2-ROS1 fusion
Concentration:

2.5, 5 and 10 μM
Incubation Time:

6 or 24 h
Result:

Induced downregulation of p-ROS1, p-AKT, p-ERK1/2, and p-STAT3 after 24 h.

In Vivo

APG-2449 (25-100 mg/kg, p.o., once daily) exerts dose-dependent antitumor activity in nude mice bearing NSCLC H3122 CDX tumors with EML4-ALK fusion^[1].
APG-2449 (25-100 mg/kg, p.o., once daily) exerts potent antitumor activity in severe combined immunodeficient (SCID) mice bearing KARPAS-299 CDX tumors with NPM-ALK fusion^[1].
APG-2449 (50-150 mg/kg, p.o., 15-22 d) exerts potent and durable antitumor activity against secondary ALK- and ROS1-resistant mutations in tumor-bearing mice model^[1].
APG-2449 (50-150 mg/kg, p.o., 22 d) shows dose-dependent antitumor activity in SCID mice bearing PA-1 CDX tumors^[1].
APG-2449 (20-60 mg/kg, p.o., 22 d) demonstrates potent antitumor activity in combination with Osimertinib (HY-15772) and Trametinib (HY-10999) in PC-9/OR xenograft models^[1].
APG-2449 (50-100 mg/kg, p.o., once daily for 2 weeks) significantly suppresses tumor growth in both KYSE-150 and KYSE-520 tumor cells xenograft models at 100 mg/kg^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Nude mice bearing NSCLC H3122 CDX tumors with EML4-ALK fusion^[1]
Dosage:

25, 50 and 100 mg/kg
Administration:

Oral gavage (p.o.), once daily
Result:

Had anti-tumor activity in a dose-dependent manner.
Did not lead to severe body weight loss.

Animal Model:

Severe combined immunodeficient (SCID) mice bearing KARPAS-299 CDX tumors with NPM-ALK fusion^[1]
Dosage:

25, 50 and 100 mg/kg
Administration:

Oral gavage (p.o.)
Result:

Exerted dose-dependent suppression of tumor phosphorylated ALK, Ak strain transforming, extracellular signal-regulated kinase and signal transducer and activator of transcription 24 hours after single dose administration.
Resulted in dose-proportional increases in APG-2449 plasma and tumor exposures.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2196186-84-0
Appearance Solid
Molecular Weight 640.24
Formel C₃₃H₄₂ClN₅O₄S
Color Off-white to light yellow
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (39.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5619 mL

7.8096 mL

15.6191 mL

5 mM

0.3124 mL

1.5619 mL

3.1238 mL

10 mM

0.1562 mL

0.7810 mL

1.5619 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (3.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (3.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.5619 mL	7.8096 mL	15.6191 mL	39.0479 mL
	5 mM	0.3124 mL	1.5619 mL	3.1238 mL	7.8096 mL
	10 mM	0.1562 mL	0.7810 mL	1.5619 mL	3.9048 mL
	15 mM	0.1041 mL	0.5206 mL	1.0413 mL	2.6032 mL
	20 mM	0.0781 mL	0.3905 mL	0.7810 mL	1.9524 mL
	25 mM	0.0625 mL	0.3124 mL	0.6248 mL	1.5619 mL
	30 mM	0.0521 mL	0.2603 mL	0.5206 mL	1.3016 mL

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APG-2449

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Membrane Protein-targeted Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

APG-2449

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Membrane Protein-targeted Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

APG-2449 Related Classifications

HY-155163 Related Classifications