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PDD00017273 is a radiosensitizing PARG) inhibitor with antitumor or activity for the study of epithelial ovaries.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $75 | In Stock | |
10 mg | $139 | In Stock | |
25 mg | $298 | In Stock | |
50 mg | $447 | In Stock | |
100 mg | $645 | In Stock | |
500 mg | $1,330 | In Stock | |
1 mL x 10 mM (in DMSO) | $88 | In Stock |
Description | PDD00017273 is a radiosensitizing PARG) inhibitor with antitumor or activity for the study of epithelial ovaries. |
Targets&IC50 | PARG:1.45 nM (Kd), PARG:26 nM |
In vitro | PDD 00017273 is an effective inhibitor of PARG with an IC50 of 26 nM and a KD of 1.45 nM. At 10 μM, PDD 00017273 does not inhibit five common cytochrome P450 enzymes. At 30 μM, it moderately increases phosphorylated H2AX (γH2AX) intensity. Additionally, PDD 00017273 reduces NAD/H through PARG inhibition after DNA damage. The compound inhibits ZR-75-1 cells carrying wild-type BRCA1 and BRCA2 and exhibits weaker activity against MDA-MB-436 cells carrying the 5396 + 1G>A mutation in BRCA1[2].At 0.3 μM, PDD 00017273 inhibits the degradation of PAR polymers in MCF7 cells. It also reduces the viability of BRCA1, BRCA2, PALB2, FAM175A, and BARD1-depleted cells. PDD 00017273 halts replication forks and induces DNA damage requiring homologous recombination (HR) for repair[1]. |
Molecular Weight | 514.62 |
Formula | C23H26N6O4S2 |
Cas No. | 1945950-21-9 |
Smiles | Cc1cc(Cn2c3ccc(cc3c(=O)n(Cc3cnc(C)s3)c2=O)S(=O)(=O)NC2(C)CC2)n(C)n1 |
Relative Density. | 1.52 g/cm3 (Predicted) |
Storage | keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 20 mg/mL (38.86 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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