Chemical Structure : TSL-1502
CAS No.:
1350723-37-3
TSL-1502
(TSL1502)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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490.56
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Formula
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C24H34N4O7
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(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
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References
1. Wang L, et al. Am J Cancer Res. 2021 Apr 15;11(4):1632-1645.
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