2798907-16-9
Chemical Structure
ITRI-90
- CAS No.: 2798907-16-9
- Formula:C45H56F3N9O6S
- Molecular Weight:908.04
InChIKey: BLWSMGOTKQNWIF-ILOPYHIUSA-N
SMILES: FC(F)(C1=NN=C2N1N=C(N3CCC(C4=CC=C(C=C4)OCCCCOCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@@H](C5)O)C(NCC6=CC=C(C7=C(N=CS7)C)C=C6)=O)=O)=O)CC3)CC2)F
Biological Activity: ITRI-90 is an orally effective androgen receptor (AR) PROTAC degrader. ITRI-90 effectively degrades full-length AR (AR-FL) and its splice variant AR-V7 proteins via the ubiquitin-proteasome system, thereby inhibiting AR transcriptional activity and the expression of its target genes, and further inducing tumor cell apoptosis. ITRI-90 can be used in research related to castration-resistant prostate cancer and Enzalutamide (HY-70002)-resistant prostate cancer[1][2].
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ITRI-90 | ITRI-90 is an orally effective androgen receptor (AR) PROTAC degrader. ITRI-90 effectively degrades full-length AR (AR-FL) and its splice variant AR-V7 proteins via the ubiquitin-proteasome system, thereby inhibiting AR transcriptional activity and the expression of its target genes, and further inducing tumor cell apoptosis. ITRI-90 can be used in research related to castration-resistant prostate cancer and Enzalutamide (HY-70002)-resistant prostate cancer. | |||||||||||||||||||||
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References
- [1]. Hung CL, et al. Targeting androgen receptor and the variants by an orally bioavailable Proteolysis Targeting Chimeras compound in castration resistant prostate cancer. EBioMedicine. 2023 Apr;90:104500. [Content Brief]
- [2]. Zhang Y, et al. PROTACs targeting androgen receptor signaling: Potential therapeutic agents for castration-resistant prostate cancer. Pharmacological research. 2024 Jul;205:107234.
