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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-DNA/RNA Synthesis-RTx-161
RTx-161

Chemical Structure : RTx-161

CAS No.: 3035072-49-9

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RTx-161 (RTx161)

货号: PC-22070Not For Human Use, Lab Use Only.

RTx-161 (RTx161) is a potent, selective, allosteric DNA Polymerase θ (Polθ) inhibitor with IC50 of 4.1 nM, exhibits preferential killing of HR-deficient cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

RTx-161 (RTx161) is a potent, selective, allosteric DNA Polymerase θ (Polθ) inhibitor with IC50 of 4.1 nM, exhibits preferential killing of HR-deficient cells.
RTx-161 shows higher potency than recently published Polθ-pol inhibitors ART558 (11.4 nM IC50) and RP6685 (6.9 nM IC50) using the identical assay.
RTx-161 shows selective killing of BRCA2-null HCT116 and DLD1 cells, with little to no effect in BRCA2-WT cells.
RTx-161 also induceds selective killing of mouse embryonic fibroblasts (MEFs) harboring a Brca1 mutation (Brca1cc/cc).
RTx-161 shows concentration dependent inhibition of Polθ-pol MMEJ activity in vitro, selectively causes DNA damage in BRCA2-null DLD1 cells, induces PARP cleavage and apoptosis.
RTx-161 exhibits strong synergistic activity with Olaparib in BRCA2-null HCT116 cells, essentially overcomes cellular resistance to Olaparib.
RTx-161 exclusively inhibits closed Polθ-pol:DNA/DNA complexes, selectively inhibits Polθ-pol in the closed state.

物理化学性质&存储条件

分子量 509.38
分子式 C21H18F7N3O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-(3-(2-hydroxyethyl)-2-oxoimidazolidin-1-yl)-4,6-bis(trifluoromethyl)phenyl (4-fluorophenyl)(methyl)carbamate

参考文献

1. Fried W, et al. Nat Commun. 2024 Apr 5;15(1):2862.

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