2101314-20-7
Chemical Structure
CX-5461 hydrochloride
- CAS No.: 2101314-20-7
- Formula:C27H28ClN7O2S
- Molecular Weight:550.07
IUPAC Name: 2-(4-methyl-1,4-diazepan-1-yl)-N-((5-methylpyrazin-2-yl)methyl)-5-oxo-5H-benzo[4,5]thiazolo[3,2-a][1,8]naphthyridine-6-carboxamide hydrochloride
InChIKey: YCGHUQKYOCALNJ-UHFFFAOYSA-N
SMILES: CC1=NC=C(N=C1)CNC(C2=C(SC3=C4C=CC=C3)N4C5=NC(N6CCN(CCC6)C)=CC=C5C2=O)=O.Cl
Biological Activity: CX-5461 hydrochloride is a selective, orally active RNA polymerase I inhibitor. CX-5461 hydrochloride disrupts the formation of the SL1-rDNA complex, thereby blocking the transcription initiation of ribosomal RNA without altering the activity of RNA polymerase II, DNA replication, or protein translation processes. CX-5461 hydrochloride upregulates the expression of p21, MDM2, Sestrin1/2, and phosphorylated AMPKα, and reduces the level of phosphorylated Akt. CX-5461 hydrochloride induces G2/G2/M cell cycle arrest, Autophagy, Apoptosis, and cellular senescence, and activates CHK1, CHK2, and RPA. CX-5461 hydrochloride can be used in research related to osteosarcoma, cervical cancer, hematologic malignancies, high-grade serous ovarian cancer, and solid tumors[1][2][3][4][5].
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CX-5461 hydrochloride | CX-5461 hydrochloride is a selective, orally active RNA polymerase I inhibitor. CX-5461 hydrochloride disrupts the formation of the SL1-rDNA complex, thereby blocking the transcription initiation of ribosomal RNA without altering the activity of RNA polymerase II, DNA replication, or protein translation processes. CX-5461 hydrochloride upregulates the expression of p21, MDM2, Sestrin1/2, and phosphorylated AMPKα, and reduces the level of phosphorylated Akt. CX-5461 hydrochloride induces G2/G2/M cell cycle arrest, Autophagy, Apoptosis, and cellular senescence, and activates CHK1, CHK2, and RPA. CX-5461 hydrochloride can be used in research related to osteosarcoma, cervical cancer, hematologic malignancies, high-grade serous ovarian cancer, and solid tumors. | |||||||||||||||||||||
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References
- [1]. Li L, et al. CX-5461 induces autophagy and inhibits tumor growth via mammalian target of rapamycin-related signaling pathways in osteosarcoma. OncoTargets and therapy. 2016;9:5985-5997. [Content Brief]
- [2]. Liu X, et al. RNA polymerase I inhibitor CX-5461 suppresses cervical cancer cell growth by inducing DNA damage and mitotic catastrophe and enhances cisplatin sensitivity. Biochemical pharmacology. 2026 Jun;248:117828. [Content Brief]
- [3]. Bywater MJ, et al. Inhibition of RNA polymerase I as a therapeutic strategy to promote cancer-specific activation of p53. Cancer cell. 2012 Jul 10;22(1):51-65. [Content Brief]
- [4]. Sanij E, et al. CX-5461 activates the DNA damage response and demonstrates therapeutic efficacy in high-grade serous ovarian cancer. Nature communications. 2020 May 26;11(1):2641.
- [5]. Drygin D, et al. Targeting RNA polymerase I with an oral small molecule CX-5461 inhibits ribosomal RNA synthesis and solid tumor growth. Cancer research. 2011 Feb 15;71(4):1418-30. [Content Brief]
