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Art. -Nr.: HY-179732

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PROTAC ALK degrader-4

PROTAC ALK degrader-4 is a ALK PROTAC degrader with a DC₅₀ of 445.25 nM. PROTAC ALK degrader-4 induces concentration- and time-dependent degradation of EML4-ALK, as well as concentration-dependent degradation of ALK^F1174L. PROTAC ALK degrader-4 downregulates 390 proteins in NCI-H3122 cells, including the targets of ceritinib (ALK, IGF-1R) and downstream molecules ERK1/2 and STAT3. PROTAC ALK degrader-4 exerts antiproliferative activity in ALK-positive cancer cells. ALK degrader-4 can be used in studies related to lung adenocarcinoma.
(Pink: Anaplastic lymphoma kinase (ALK) ligand (HY-15656); Blue: Cereblon ligand (HY-179733); Black: linker).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₄₆H₆₃ClN₈O₇S
Molecular Weight:907.56

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

PROTAC ALK degrader-4 Chemical Structure

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Preis

Verfügbarkeit

Menge

Amount: USD 0.00

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

PROTAC ALK degrader-4 is a ALK PROTAC degrader with a DC₅₀ of 445.25 nM. PROTAC ALK degrader-4 induces concentration- and time-dependent degradation of EML4-ALK, as well as concentration-dependent degradation of ALK^F1174L. PROTAC ALK degrader-4 downregulates 390 proteins in NCI-H3122 cells, including the targets of ceritinib (ALK, IGF-1R) and downstream molecules ERK1/2 and STAT3. PROTAC ALK degrader-4 exerts antiproliferative activity in ALK-positive cancer cells. ALK degrader-4 can be used in studies related to lung adenocarcinoma^[1]. (Pink: Anaplastic lymphoma kinase (ALK) ligand (HY-15656); Blue: Cereblon ligand (HY-179733); Black: linker).

IC₅₀ & Target

^[1]

EML4-ALK

445.25 nM (DC₅₀)

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle ERK Isoform-spezifische Produkte anzeigen :

Alle STAT Isoform-spezifische Produkte anzeigen :

In Vitro

PROTAC ALK degrader-4 (compound B8) (0.1-10000 nM; 1-48 h) induces CRBN- and ubiquitin-proteasome system-dependent degradation of EML4-ALK in NCI-H3122 cells in a dose- and time-dependent manner, with a DC₅₀ of 445.25 nM^[1].
PROTAC ALK degrader-4 induces concentration-dependent degradation of the ALK^F1174L mutant in Kelly cells, and exhibits non-mutant-selective ALK degradation activity^[1].
PROTAC ALK degrader-4 (24 h) exerts antiproliferative activity in NCI-H2228 and NCI-H3122 cells^[1].
PROTAC ALK degrader-4 (500 nM; 24 h) causes significant downregulation of 390 proteins in NCI-H3122 cells, including ceritinib kinase targets such as ALK and IGF-1R, as well as their downstream pathway proteins ERK1/2 and STAT3 ^[1].

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

Western Blot Analysis^[1]

Cell Line:

NCI-H3122 cells
Concentration:

0.1, 1, 10, 100, 1000 and 10000 nM
Incubation Time:

24 h
Result:

It induced EML4-ALK in NCI-H3122 cells, with a DC50 of 445.25 nM.

Western Blot Analysis^[1]

Cell Line:

NCI-H3122 cells
Concentration:

100 nM
Incubation Time:

1, 2, 4, 8, 12, 24 and 48 h
Result:

Time-dependent degradation of EML4-ALK was induced in NCI-H3122 cells

Chemical Information

Molecular Weight 907.56
Formel C₄₆H₆₃ClN₈O₇S
SMILES

CC1=CC(NC2=NC(NC3=CC=CC=C3S(=O)(C(C)C)=O)=C(C=N2)Cl)=C(C=C1C4CCN(CC4)CCCCCCCC(NC5(CCC5)C(NC6C(NC(CC6)=O)=O)=O)=O)OC(C)C
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 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]. Huang K, et al. Design, synthesis, and biological evaluation of novel PROTACs based on unnatural dipeptide CRBN ligands. European journal of medicinal chemistry. 2026 Feb 05;303:118387. [Content Brief]

Calculators

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)}

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.

Bioz

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

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PROTAC ALK degrader-4

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle ERK Isoform-spezifische Produkte anzeigen

Alle STAT Isoform-spezifische Produkte anzeigen