CRBN ligand-898
CRBN ligand-898 is a CRBN ligand with a Kd of 216 nM. CRBN ligand-898 binds to CRBN, and when incorporated into proteolysis targeting chimeras (PROTACs), mediates degradation of intended target proteins. CRBN ligand-898 does not induce degradation of IMiD-associated neosubstrates Ikaros (IKZF1) and Aiolos (IKZF3). CRBN ligand-898 can be used to synthesize PROTACs.
For research use only. We do not sell to patients.
- CAS No.: 2766178-72-5
- Formula: C12H11N3O2
- Molecular Weight:229.23
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cereblon 216 nM (Kd) |
Cereblon 183 nM (IC50) |
CRBN ligand-898 (Compound 2) binds to CRBN with an IC50 of 183 nM and a Kd of 216 nM[1].
CRBN ligand-898 does not inhibit hERG, NaV1.5, Kv4.3 with IC50 >40 μM, or CaV (IC50 >100 μM) ion channels, and does not induce cytotoxicity in THP-1 cells (IC50 >250 μM)[1].
CRBN ligand-898 (1-10 μM; 24 h) does not degrade Ikaros or Aiolos in NB-4 human leukaemia cells[1].
CRBN ligand-898 (0.0001-30 μM; 6 h) dose-dependently inhibits IMiD- and PROTAC-induced Aiolos degradation in HiBiT-IKZF3 MM.1S cells, confirming CRBN engagement and cell permeability[1].
CRBN ligand-898 (1 μM; 24 h) does not reduce levels of any proteins, including IMiD neosubstrates, in NB-4 human leukaemia cells when treated at 1 μM for 24 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NB-4 human leukaemia cells
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Concentration:1, 10 μM
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Incubation Time:24 h
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Result:Did not reduce protein levels of Ikaros or Aiolos at either tested concentration.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CrbnI391V knock C57BL/6N (wild-type)[1]
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Dosage:10 mg/kg; 30 mg/kg; 100 mg/kg
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Administration:p.o.; single dose
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Result:Showed no degradation of Ikaros or Aiolos in spleen tissue.
Exhibited dose-dependent increases in plasma Cmax, reaching 250 µmol/L at 100 mg/kg.
Exhibited dose-dependent increases in plasma AUC, reaching 800 µmol·h/L at 100 mg/kg.
Chemical Information
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CAS No. 2766178-72-5
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Molecular Weight 229.23
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Formula C12H11N3O2
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SMILES
O=C1NC(CCN1C2=CC3=C(C=CN3)C=C2)=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)
CRBN ligand-898 Related Classifications
HY-W947273 Related Classifications
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