2. Protein Tyrosine Kinase/RTK Apoptosis
  3. ROS Kinase FAK Anaplastic lymphoma kinase (ALK) Apoptosis
  4. 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.

For research use only. We do not sell to patients.

APG-2449 Chemical Structure

APG-2449 Chemical Structure

CAS No. : 2196186-84-0

Size Price Stock Quantity
Free Sample (0.1 - 0.2 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

APG-2449 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

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.

APG-2449 Related Antibodies

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
Molecular Weight

640.24

Formula

C33H42ClN5O4S
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5619 mL 7.8096 mL 15.6191 mL
5 mM 0.3124 mL 1.5619 mL 3.1238 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.93%

SDS (251 KB)

COA (249 KB) HNMR (150 KB) RP-HPLC (169 KB) LCMS (107 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

APG-2449 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

APG-24492196186-84-0APG2449APG 2449ROS KinaseFAKAnaplastic lymphoma kinase (ALK)ApoptosisPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246ESCCcancertumorNSCLCInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
APG-2449
Cat. No.:
HY-155163
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

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) Portuguese - PT (251 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.