CCT-367766|PROTACs|CAS 2229856-58-8|DC Chemicals

Cas No.:	2229856-58-8
Chemical Name:	N-(2-Chloro-5-(2,3-dihydrobenzo[b][1,4]dioxine-6-carboxamido)phenyl)-2-((4-(2-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)ethoxy)ethoxy)ethyl)piperazin-1-yl)methyl)quinoline-6-carboxamide
Synonyms:	CCT367766;CCT 367766
SMILES:	N1C2C(=CC(C(NC3=CC(NC(C4=CC=C5C(=C4)OCCO5)=O)=CC=C3Cl)=O)=CC=2)C=CC=1CN1CCN(CCOCCOCCOC2=CC=CC3=C2C(=O)N(C2CCC(=O)NC2=O)C3=O)CC1
Formula:	C₄₉H₄₈ClN₇O₁₁
M.Wt:	946.41
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[1]. Chessum NEA, et al. Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766).J Med Chem. 2018 Feb 8;61(3):918-933.

Description:	CCT-367766 (CCT367766) is a novel heterobifunctional PROTAC that binds and degrades the putative transcription factor regulator Pirin in cells.
Target:	CRBN-DDB1:490 nM (IC50)
In Vitro:	CCT367766 (50-1500 nM; 24 hours) demonstates the depletion of pirin protein as a the time-dependent hook-effect in SK-OV-3 human ovarian cancer cells[1]. CCT367766 (0.5-50 nM; 2 hours) demonstrates the concentration-dependent depletion of pirin protein after 2 h exposure in SK-OV-3 cells[1]. Western Blot Analysis[1] Cell Line: SK-OV-3 human ovarian cancer cells Concentration: 50, 150, 250, 500 and 1500 nM Incubation Time: 2 hours, 4 hours, 24 hours Result: Decreased pirin protein expression. Western Blot Analysis[1] Cell Line: SK-OV-3 human ovarian cancer cells Concentration: 0.5, 1, 2.5, 5, 7.5, 10, 25, and 50 nM Incubation Time: 2 hours Result: Completely degraded pirin just at 50 nM treatment.
References:	[1]. Chessum NEA, et al. Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766).J Med Chem. 2018 Feb 8;61(3):918-933.

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