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))
(Pink: Btk and IKZF1 and IKZF3 ligand (HY-179076); Blue: Cereblon ligand (HY-41547); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 2416130-49-7
- Formula: C43H51N11O6
- Molecular Weight:817.94
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
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Biological Activity
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IKZF1 |
IKZF3 |
Cereblon |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-week-old female NOD-SCID mice bearing OCI-ly1 xenografts[1]
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Dosage:3 and 10 mg/kg
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Administration:Orally administration, daily for 21 days
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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.
Chemical Information
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CAS No. 2416130-49-7
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Molecular Weight 817.94
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Formula C43H51N11O6
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)