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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-PARP-TSL-1502
TSL-1502

Chemical Structure : TSL-1502

CAS No.: 1350723-37-3

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TSL-1502 (TSL1502)

货号: PC-27716Not For Human Use, Lab Use Only.

TSL-1502 is a glucuronide prodrug of poly (ADP-ribose) polymerase (PARP) inhibitor TSL-1502M, which is a potent PARP1 and PARP2 inhibitor with IC50 of 0.66 nM and 0.87 nM respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

TSL-1502 is a glucuronide prodrug of poly (ADP-ribose) polymerase (PARP) inhibitor TSL-1502M, which is a potent PARP1 and PARP2 inhibitor with IC50 of 0.66 nM and 0.87 nM respectively.
TSL-1502 prodrug has no activity on PARP1 and PARP2.
TSL-1502 could release the active parent drug TSL-1502M in cells.
TSL-1502 induces persistent DSBs, G2/M arrest and apoptosis in HR-deficient cells, and displays stronger effects than olaparib.
TSL-1502 selectively inhibits the proliferation of HR-deficient cancer cells.
TSL-1502M sensitizes both HR-deficient and HR-proficient cancer cells to conventional chemotherapy
TSL-1502 at 25 and 50 mg/kg (p.o., BID×14) exhibited profound anti-tumor activity in MX-1 (BRCA1-deficient, BRCA2-mutated) xenografts model, sensitized irinotecan anti-tumor effect.

物理化学性质&存储条件

分子量 490.56
分子式 C24H34N4O7
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

(2S,3S,4S,5R,6S)-3,4,5-trihydroxy-6-((3-methyl-1-((S)-1-propylpyrrolidin-3-yl)-6,7,8,9-tetrahydro-3H-pyrazolo[3,4-c]isoquinolin-5-yl)oxy)tetrahydro-2H-pyran-2-carboxylic acid

参考文献

1. Wang L, et al. Am J Cancer Res. 2021 Apr 15;11(4):1632-1645.

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