N-piperidine Ibrutinib

TargetMol
Product Code: TAR-T9408
Supplier: TargetMol
CodeSizePrice
TAR-T9408-1mg1mg£189.00
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TAR-T9408-5mg5mg£340.00
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TAR-T9408-10mg10mg£466.00
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TAR-T9408-25mg25mg£705.00
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TAR-T9408-50mg50mg£970.00
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TAR-T9408-100mg100mg£1,267.00
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Overview

Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃

Images

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Further Information

Bioactivity:
N-piperidine Ibrutinib is a potent BTK inhibitor with IC50s of 51.0 for WT BTK and 30.7 nM for C481S BTK respectively. N-piperidine Ibrutinib can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620. SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM.
CAS:
330785-90-5
Formula:
C22H22N6O
Molecular Weight:
386.45
Pathway:
Tyrosine Kinase/Adaptors; Angiogenesis
Purity:
0.9665
SMILES:
Nc1c(c(-c(cc2)ccc2Oc2ccccc2)nn2C3CCNCC3)c2ncn1
Target:
BTK

References

Jaime-Figueroa S, et al. Design, synthesis and biological evaluation of Proteolysis Targeting Chimeras (PROTACs) as a BTK degraders with improved pharmacokinetic properties. Bioorg Med Chem Lett. 2020 Feb 1;30(3):126877. Buhimschi AD, et al. Targeting the C481S Ibrutinib-Resistance Mutation in Bruton's Tyrosine Kinase Using PROTAC-Mediated Degradation. Biochemistry. 2018 Jul 3;57(26):3564-3575.