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
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M.Wt
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1087.75
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Formula
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C52H67ClN12O8S2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Sarott RC, et al. Science. 2024 Oct 4;386(6717):eadl5361.
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