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CDK-TCIP2

Chemical Structure : CDK-TCIP2

CAS No.:

CDK-TCIP2

Catalog No.: PC-23151Not For Human Use, Lab Use Only.

CDK-TCIP2 is a bivalent molecule linking CDK9 inhibitor SNS-032 to BCL6 ligand BI3812, activates BCL6-regulated transcription, potently and specifically kills BCL6-overexpressing cells with EC50 of 0.9 nM for SUDHL5 cells.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

CDK-TCIP2 is a bivalent molecule linking CDK9 inhibitor SNS-032 to BCL6 ligand BI3812, activates BCL6-regulated transcription, potently and specifically kills BCL6-overexpressing cells with EC50 of 0.9 nM for SUDHL5 cells.
CDK-TCIP2 exhibits improved metabolic stability and higher concentrations in blood than CDK-TCIP1 (Cat# PC-23150) after intraperitoneal dosing, permitting its use in vivo.
CDK-TCIP2 (10 mg/kg once daily, 5 mg/kg twice daily) specifically suppresses the proliferation of GC B cells in a mouse immunization model.

Physicochemical Properties

M.Wt 1087.75
Formula C52H67ClN12O8S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(5-(((5-(tert-butyl)oxazol-2-yl)methyl)thio)thiazol-2-yl)-1-(2-(9-(1-(5-chloro-4-((8-methoxy-1-methyl-3-(2-(methylamino)-2-oxoethoxy)-2-oxo-1,2-dihydroquinolin-6-yl)amino)pyrimidin-2-yl)piperidine-4-carbonyl)-3,9-diazaspiro[5.5]undecan-3-yl)-2-oxoethyl)piperidine-4-carboxamide

References

1. Sarott RC, et al. Science. 2024 Oct 4;386(6717):eadl5361.

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