2869057-11-2
Chemical Structure
WWL0245
- CAS No.: 2869057-11-2
- Formula:C45H51N11O8
- Molecular Weight:873.96
IUPAC Name: 4-(((R)-5-(cyclohexylmethyl)-4-ethyl-1-methyl-4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridin-7-yl)amino)-N-(1-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetyl)piperidin-4-yl)-3-methoxybenzamide
InChIKey: AORZPRLVKUMTOJ-XGDNGBMYSA-N
SMILES: CC[C@@H](N(C1=N2)CC3CCCCC3)C4=NN=C(C)N4C1=CN=C2NC5=C(C=C(C=C5)C(NC6CCN(CC6)C(COC7=C8C(C(N(C9C(NC(CC9)=O)=O)C8=O)=O)=CC=C7)=O)=O)OC
Biological Activity: WWL0245 is a potent and seletive BRD4 PROTAC. WWL0245 selectively degrades BRD4 with sub-nanomolar DC50 (<1 nM) than BRD2/3 and PLK1 ( DC50>1 μM). WWL0245 shows excellent selective cytotoxicity in the BETi sensitive cancer cell lines, including AR-positive prostate cancer cell lines. WWL0245 is a promising drug candidate for AR-positive prostate cancer research and a valuable tool compound to study the biological function of BRD4[1].
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WWL0245 | WWL0245 is a potent and seletive BRD4 PROTAC. WWL0245 selectively degrades BRD4 with sub-nanomolar DC50 (<1 nM) than BRD2/3 and PLK1 ( DC50>1 μM). WWL0245 shows excellent selective cytotoxicity in the BETi sensitive cancer cell lines, including AR-positive prostate cancer cell lines. WWL0245 is a promising drug candidate for AR-positive prostate cancer research and a valuable tool compound to study the biological function of BRD4. | |||||||||||||||||||||
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Keywords
