1. PROTAC Protein Tyrosine Kinase/RTK Immunology/Inflammation
  2. PROTACs Btk IKZF Family
  3. PROTAC BTK/IKZF1/3 Degrader-1

PROTAC BTK/IKZF1/3 Degrader-1 is a selective and orally active BCL6 and IKZF1/3 PROTAC degrader. PROTAC BTK/IKZF1/3 Degrader-1 exhibits antitumor activity. PROTAC BTK/IKZF1/3 Degrader-1 can be used for the research of cancer, such as lymphoma. (Structure Note: Pink: BCL6/IKZF1/3 ligand (HY-179076); Blue: CRBN ligand (HY-41547))

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

PROTAC BTK/IKZF1/3 Degrader-1

PROTAC BTK/IKZF1/3 Degrader-1 Chemical Structure

CAS No. : 2416130-49-7

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Description

PROTAC BTK/IKZF1/3 Degrader-1 is a selective and orally active BCL6 and IKZF1/3 PROTAC degrader. PROTAC BTK/IKZF1/3 Degrader-1 exhibits antitumor activity. PROTAC BTK/IKZF1/3 Degrader-1 can be used for the research of cancer, such as lymphoma[1]. (Structure Note: Pink: BCL6/IKZF1/3 ligand (HY-179076); Blue: CRBN ligand (HY-41547))

IC50 & Target[1]

IKZF1

 

IKZF3

 

Cereblon

 

In Vitro

PROTAC BTK/IKZF1/3 Degrader-1 (Compound BT6) (1-300 nM, 24 h) concentration-dependently degrades BTK and IKZF1/3 proteins (BTK degradation rate exceeds 75% at 33.3 nM, IKZF1/3 degradation rate exceeds 50% at 300 nM) in diffuse large B-cell lymphoma (DLBCL) cells including Mino and OCI-ly10[1].

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

In Vivo

PROTAC BTK/IKZF1/3 Degrader-1 ( Compound BT6) (1-300 nM, 24 h) (3-10 mg/kg, p.o., daily for 21 days) significantly inhibits tumor growth with tumor growth in NOD-SCID mice bearing OCI-ly10 xenografts[1].

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

Animal Model: 6-week-old female NOD-SCID mice bearing OCI-ly1 xenografts[1]
Dosage: 3 and 10 mg/kg
Administration: Orally administration, daily for 21 days
Result: Showed tumor growth inhibition (TGI) rates of 95.54% and 115.72%.
Degraded BTK and IKZF1/3 proteins in tumor tissues.
Showed no significant body weight changes.
Molecular Weight

817.94

Formula

C43H51N11O6

CAS No.
SMILES

CN1CCN(C1=O)[C@@H]2CCCN(C2)C3=CN=C(C(NC4=CC=C(C=C4)C5CCN(CC5)CC6CCN(C6)C7=CC8=C(C(N(C8=O)C9CCC(NC9=O)=O)=O)C=C7)=N3)C(N)=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:
PROTAC BTK/IKZF1/3 Degrader-1
Cat. No.:
HY-179077
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