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
Description
IC50 & Target
[1]|
Cereblon 216 nM (Kd) |
Cereblon 183 nM (IC50) |
In Vitro
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.
In Vivo
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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