2. PROTAC Protein Tyrosine Kinase/RTK Apoptosis
  3. PROTACs Src Btk Apoptosis
  4. DFCI-002-06

DFCI-002-06 is an orally active dual-target HCK/BTK PROTAC degrader with DC₅₀ values for HCK and BTK of 1.3 and 4.5 nM respectively. DFCI-002-06 retains higher anti-tumor activity than the HCK/BTK dual-target inhibitor (HY-15805), inducing apoptosis in cancer cells. DFCI-002-06 can be used for the study of MYD88 mutant B-cell malignancies.
(Pink: Src and Btk ligand (HY-15805); Blue: Cereblon ligand (HY-W087383); Black: linker).

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

DFCI-002-06

DFCI-002-06 Chemical Structure

CAS No. : 3092208-36-8

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DFCI-002-06 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Lck Fyn Blk Fgr Hck Lyn Yes SRC-3

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Description

DFCI-002-06 is an orally active dual-target HCK/BTK PROTAC degrader with DC₅₀ values for HCK and BTK of 1.3 and 4.5 nM respectively. DFCI-002-06 retains higher anti-tumor activity than the HCK/BTK dual-target inhibitor (HY-15805), inducing apoptosis in cancer cells. DFCI-002-06 can be used for the study of MYD88 mutant B-cell malignancies[1]. (Pink: Src and Btk ligand (HY-15805); Blue: Cereblon ligand (HY-W087383); Black: linker).

IC50 & Target[1]

Hck

1.3 nM (DC50)

Cereblon

 

Molecular Weight

794.90

Formula

C44H46N10O5
CAS No.
SMILES

NC1=C2C(N([C@@H]3CC[C@@H](N4CCN(CC5CN(C6=CC7=C(C(N(C(CC8)C(NC8=O)=O)C7=O)=O)C=C6)C5)CC4)CC3)N=C2C9=CC=C(OC%10=CC=CC=C%10)C=C9)=NC=N1
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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
References
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DFCI-002-06 Related Classifications

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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:

DFCI-002-063092208-36-8PROTACsSrcBtkApoptosisBruton tyrosine kinasePROTACHCKBTKMYD88 mutationtargeted protein degradationWaldenstrom's macroglobulinemiaB-cell malignancieskinase inhibitor resistanceInhibitorinhibitorinhibit

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HY-181050
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