2760703-21-5
Chemical Structure
TD-802
- CAS No.: 2760703-21-5
- Formula:C52H61ClN10O6
- Molecular Weight:957.56
IUPAC Name: (E)-N-(2-((1H-indol-5-yl)amino)-2-oxoethyl)-3-(4-hydroxy-3-methoxyphenyl)acrylamide
InChIKey: DWMRQCSGBKQGKE-HVMYGMEOSA-N
SMILES: CC1([C@@H](C(C)([C@H]1OC2=CC(Cl)=C(C=C2)C#N)C)NC(C3=CC=C(C=C3)N4CCN(CC4)C5CC6(C5)CCN(CC6)C(C7CCN(CC7)C8=CC=C9N=NN(C(C9=C8)=O)C%10CCC(NC%10=O)=O)=O)=O)C
Biological Activity: TD-802 is a CRBN-recruiting PROTAC androgen receptor (AR) degrader with liver microsomal stability and in vivo pharmacokinetic properties. TD-802 exhibits weak degrading activity against the AR-V7 splice variant, and its degradation process depends on the ubiquitin-proteasome system and Cullin-Ring ubiquitin ligase. TD-802 inhibits the proliferation of AR-dependent prostate cancer cells and the growth of AR-positive prostate cancer tumors in in vivo xenograft models[1].
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TD-802 | TD-802 is a CRBN-recruiting PROTAC androgen receptor (AR) degrader with liver microsomal stability and in vivo pharmacokinetic properties. TD-802 exhibits weak degrading activity against the AR-V7 splice variant, and its degradation process depends on the ubiquitin-proteasome system and Cullin-Ring ubiquitin ligase. TD-802 inhibits the proliferation of AR-dependent prostate cancer cells and the growth of AR-positive prostate cancer tumors in in vivo xenograft models. | |||||||||||||||||||||
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Keywords
