1. PROTAC Protein Tyrosine Kinase/RTK
  2. HyT Anaplastic lymphoma kinase (ALK)
  3. ALK degrader 3

ALK degrader 3 is a ALK HyT degrader with an IC50 of 1.2 nM. ALK degrader 3 inhibits ALK kinase activity, increases the solvent-accessible surface area of hydrophobic residues near the ALK binding pocket, promotes ALK to form a partially unfolded conformation, and drives ALK degradation via the proteasomal pathway. ALK degrader 3 inhibits the proliferation of tumor cells. ALK degrader 3 can be used for the research of non-small cell lung cancer. (ALK ligand: Brigatinib (HY-12857); hydrophobic tag: Tetraasterane (HY-W1139353)).

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

ALK degrader 3

ALK degrader 3 Chemical Structure

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Description

ALK degrader 3 is a ALK HyT degrader with an IC50 of 1.2 nM. ALK degrader 3 inhibits ALK kinase activity, increases the solvent-accessible surface area of hydrophobic residues near the ALK binding pocket, promotes ALK to form a partially unfolded conformation, and drives ALK degradation via the proteasomal pathway. ALK degrader 3 inhibits the proliferation of tumor cells. ALK degrader 3 can be used for the research of non-small cell lung cancer. (ALK ligand: Brigatinib (HY-12857); hydrophobic tag: Tetraasterane (HY-W1139353))[1].

In Vitro

ALK degrader 3 (compound B10) potently inhibits the proliferation of H3122 cells after 7 days, with an IC50 of 97.77 nM[1].
ALK degrader 3 (0.05-2 μM; 24 h) induces concentration-dependent degradation of ALK protein in H3122 cells[1].

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

Western Blot Analysis[1]

Cell Line: H3122 cells
Concentration: 0.05, 0.1, 0.5, 1, 2 μM
Incubation Time: 24 h
Result: Reduced ALK levels in a concentration-dependent manner.
Molecular Weight

930.42

Formula

C47H57ClN7O9P

SMILES

CP(C)(C1=CC=CC=C1NC2=NC(NC3=CC=C(N4CCC(N5CCN(C(C67C(CC8C9C7)(C(OC)=O)C%10C6CC9(C(OC)=O)C8(C(OC)=O)C%10)=O)CC5)CC4)C=C3OC)=NC=C2Cl)=O

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
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  • 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.

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Product Name:
ALK degrader 3
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HY-182087
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