BSJ-04-132

Modify Date: 2024-01-14 20:20:09

BSJ-04-132 Structure
BSJ-04-132 structure
Common Name BSJ-04-132
CAS Number 2349356-39-2 Molecular Weight 819.91
Density N/A Boiling Point N/A
Molecular Formula C42H49N11O7 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of BSJ-04-132


BSJ-04-132 is a potent and selective Ribociclib-based CDK4 degrader (PROTAC), with IC50s of 50.6 nM and 30 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-04-132 does not induce CDK6 and IKZF1/3 degradation. BSJ-04-132 has anti-cancer activity[1].

 Names

Name BSJ-04-132

 BSJ-04-132 Biological Activity

Description BSJ-04-132 is a potent and selective Ribociclib-based CDK4 degrader (PROTAC), with IC50s of 50.6 nM and 30 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-04-132 does not induce CDK6 and IKZF1/3 degradation. BSJ-04-132 has anti-cancer activity[1].
Related Catalog
Target

CDK4/D1:50.6 nM (IC50)

CDK6/D1:30 nM (IC50)

In Vitro BSJ-04-132 (0.1-5 μM; for 4 hours) only resultes in degradation of CDK4 in WT cells, not CDK6 and IKZF1/3[1]. Western Blot Analysis[1] Cell Line: Wildtype (WT) or Crbn-/- Jurkat cells Concentration: 0.1, 0.5, 1, 5 μM Incubation Time: For 4 hours Result: Only resulted in degradation of CDK4 in WT cells, not CDK6 and IKZF1/3.
References

[1]. Baishan Jiang, et al. Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6. Angew Chem Int Ed Engl. 2019 May 6;58(19):6321-6326.

 Chemical & Physical Properties

Molecular Formula C42H49N11O7
Molecular Weight 819.91

 Safety Information

Hazard Codes Xi