IKZF2-degrader 1
IKZF2-degrader 1 is a potent and selective molecular glue degrader that selectively degrades IKZF2, with DC50 values of 0.6 nM and 2.0 nM in HEK293T cells and Jurkat cells, respectively. IKZF2-degrader 1 exerts no degrading effect on CK1α, IKZF1 and GSPT1, and shows weak activity against IKZF3. IKZF2-degrader 1 can be used in studies related to IKZF2-dependent cancers.
For research use only. We do not sell to patients.
- CAS No.: 2983840-43-1
- Formula: C27H30FN7O3
- Molecular Weight:519.57
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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]|
IZKF2 0.6 nM (DC50, HEK293T HiBiT) |
IZKF2 2 nM (DC50, Jurkat FACS) |
In Vitro
IKZF2-degrader 1 (compound 31) potently degrades IKZF2 in the IKZF2 HiBiT degradation assay in HEK293T cells, with a DC50 of 0.6 nM and a Dmax of 86%; it exhibits significantly weaker degradation activity against CK1α, with a DC50 of 210 nM and a Dmax of 23%[1].
IKZF2-degrader 1 potently and efficiently degrades IKZF2 in Jurkat cells, with a DC50 of 2.0 nM and a Dmax of 90%[1].
IIKZF2-degrader 1 exhibits good degradation selectivity toward other novel CRBN substrates. It shows no significant degradation activity against IKZF1 and GSPT1 (DC50 > 10 μM; Dmax < 20%), weak degradation activity against IKZF3 (DC50 = 89 nM; Dmax = 34%), and is capable of degrading SALL4 (DC50 = 1.8 nM; Dmax = 61%)[1].
The metabolic stability T1/2 of IKZF2-degrader 1 in human, cynomolgus monkey, rat and mouse liver microsomes is 140, 40, 71 and 72 min, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 mice[1]
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Dosage:1 mg/kg (i.v.); 3 mg/kg (p.o.)
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Administration:i.v.; single dose; p.o.; single dose
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Result:Exhibited a half-life of 3.0 h, clearance of 103 mL/min/kg, and volume of distribution at steady state of 1.26 L/kg.
Exhibited a half-life of 2.8 h, maximum plasma concentration of 60 ng/mL, area under the curve of 101 h*ng/mL, and oral bioavailability of 22%.
Chemical Information
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CAS No. 2983840-43-1
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Molecular Weight 519.57
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Formula C27H30FN7O3
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SMILES
CC(C)NC1=NNC2=C(CN3CCCC3)C=C(C4=C(F)C(CN(C5CCC(NC5=O)=O)C6=O)=C6C=C4)N=C21
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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)
IKZF2-degrader 1 Related Classifications
HY-172882 Related Classifications
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