2. Protein Tyrosine Kinase/RTK Apoptosis
  3. Anaplastic lymphoma kinase (ALK) Apoptosis
  4. ALK-IN-37

ALK-IN-37 is an orally active type I1/2 allosteric inhibitor of anaplastic lymphoma kinase (ALK) with an IC50 of 9.58 nM. ALK-IN-37 induces cell apoptosis, inhibits colony formation, suppresses cell migration, and exerts antiproliferative effects in cancer cells overexpressing ALK. ALK-IN-37 can be used in research related to non-small cell lung cancer.

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

ALK-IN-37

ALK-IN-37 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

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

ALK-IN-37 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

ALK-IN-37 is an orally active type I1/2 allosteric inhibitor of anaplastic lymphoma kinase (ALK) with an IC50 of 9.58 nM. ALK-IN-37 induces cell apoptosis, inhibits colony formation, suppresses cell migration, and exerts antiproliferative effects in cancer cells overexpressing ALK. ALK-IN-37 can be used in research related to non-small cell lung cancer[1].

In Vitro

ALK-IN-37 (Compound C04) (48 h) selectively inhibits the proliferation of ALK-overexpressing H2228 cells (IC50 = 0.10 μM) and ALK-positive Karpas299 cells (IC50 = 0.53 μM), shows weak activity against ALK-negative A549 cells, and exhibits no activity against WML2 cells[1].
ALK-IN-37 (50-200 nM; 14 days) dose-dependently inhibits colony formation of H2228 cells, with 200 nM reducing the colony formation efficiency to 36.3%[1].
ALK-IN-37 (50-200 nM; 24-48 h) inhibits the migration of H2228 cells in a dose-dependent manner, and a concentration of 200 nM reduces the 48-hour scratch wound healing rate to 28.5%[1].
ALK-IN-37 (100-200 nM; 24 h) inhibits the invasion of H2228 cells in a dose-dependent manner, with 200 nM reducing the relative invasion area to 36.6%[1].
ALK-IN-37 (50-200 nM; 24 h) induces G0/G1 cell cycle arrest in H2228 cells in a dose-dependent manner, and treatment with 200 nM increases the proportion of G0/G1 phase cells to 85.0%[1].
ALK-IN-37 (50-200 nM; 24 h) induces apoptosis in H2228 cells in a dose-dependent manner, and treatment with 200 nM increases the proportion of apoptotic cell population to 55.9%[1].
ALK-IN-37 (50-200 nM) dose-dependently inhibits the phosphorylation of ALK and the downstream STAT3/AKT signaling pathway in H2228 cells, with the strongest inhibitory effect observed at 200 nM[1].

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

ALK-IN-37 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: H2228
Concentration: 50, 100 and 200 nM
Incubation Time: 14 days, medium refreshed every 3 days
Result: Dose-dependently suppressed colony formation efficiency, reducing it to 82.0%, 48.3%, and 36.3% at 50, 100, and 200 nM respectively.

Cell Migration Assay [1]

Cell Line: H2228
Concentration: 50, 100 and 200 nM
Incubation Time: 24 h, 48 h
Result: Dose-dependently impeded wound closure at both 24 and 48 h.
Reduced 48-h wound closure to 44.7% in the 100 nM group and 28.5% in the 200 nM group.

Cell Invasion Assay[1]

Cell Line: H2228
Concentration: 100 and 200 nM
Incubation Time: 24 h
Result: Dose-dependently inhibited H2228 cell invasion, reducing relative invasion area to 50.4% at 100 nM and 36.6% at 200 nM.

Cell Cycle Analysis[1]

Cell Line: H2228
Concentration: 50, 100 and 200 nM
Incubation Time: 24 h
Result: Dose-dependently induced G0/G1 phase cell cycle arrest.
Increased the proportion of cells in G0/G1 phase from 54.3% in the control to 61.6%, 72.5%, and 85.0% at 50, 100, and 200 nM respectively, with corresponding decreases in S and G2/M phase populations.

Apoptosis Analysis[1]

Cell Line: H2228
Concentration: 50, 100 and 200 nM
Incubation Time: 24 h
Result: Dose-dependently induced apoptosis in H2228 cells.
Increased the percentage of apoptotic cells from 5.4% in the control to 24.6%, 30.0%, and 55.9% at 50, 100, and 200 nM respectively.
In Vivo

ALK-IN-37 (Compound C04) (10-30 mg/kg; p.o.; daily; 15 days) exhibits dose-dependent, potent anti-tumor efficacy and on-target ALK inhibition in BALB/c nude mice with H2228 NSCLC xenografts, with superior activity to crizotinib at 30 mg/kg[1].

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

Animal Model: BALB/c nude (female)[1]
Dosage: 10 mg/kg; 20 mg/kg; 30 mg/kg
Administration: p.o.; daily; 15 days
Result: Showed dose-dependent inhibition of tumor growth, with significantly reduced tumor weights in all treated groups compared to vehicle control.
Reduced relative p-ALK/ALK levels to ~85% of vehicle control at 10 mg/kg, ~70% at 20 mg/kg, and ~35% at 30 mg/kg, with greater reduction than 30 mg/kg crizotinib.
Reduced p-ALK positive area to ~30% of vehicle control at 10 mg/kg, ~18% at 20 mg/kg, and ~8% at 30 mg/kg, with greater reduction than 30 mg/kg crizotinib.
Showed no significant body weight differences compared to vehicle control and no treatment-related pathological lesions in major organs.
Molecular Weight

344.37

Formula

C19H16N6O
SMILES

O=C(C1=CC(C2=CC=CC(N3C=NN=C3)=C2)=NN1)NC4=CC=CC(C)=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • 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.

ALK-IN-37 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

ALK-IN-37Anaplastic lymphoma kinase (ALK)ApoptosisAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246ALK-overexpressing cancer cellsNSCLC xenograftsSTAT3/AKT signalingBALB/c nude miceA549 cellsWML2 cellsH2228 cellsanaplastic lymphoma kinaseKarpas299 cellsnon-small cell lung cancerInhibitorinhibitorinhibit

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:
ALK-IN-37
Cat. No.:
HY-183358
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)

Request for HNMR Report

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