PDD 00017272

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Cat.No. 7006 - PDD 00017272 | C23H25N5O4S3 | CAS No. 1945950-20-8
Description: Potent PARG inhibitor
Chemical Name: 1-[(2,4-Dimethyl-5-thiazolyl)methyl]-1,2,3,4-tetrahydro-N-(1-methylcyclopropyl)-3-[(2-methyl-5-thiazolyl)methyl]-2,4-dioxo-6-quinazolinesulfonamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (1)

Biological Activity

Potent poly (ADP ribose) glycohydrolase (PARG) inhibitor (IC50 values are 4.8 nM in biochemical assay and 9.2 nM in cell based assay).

Licensing Information

Sold under license from Cancer Research Technology Ltd (Ximbio).

Technical Data

M. Wt 531.66
Formula C23H25N5O4S3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1945950-20-8
PubChem ID 134169694
InChI Key QOEXRJYTAZZRPL-UHFFFAOYSA-N
Smiles CC1=NC=C(S1)CN2C(N(C3=CC=C(S(=O)(NC4(CC4)C)=O)C=C3C2=O)CC5=C(N=C(S5)C)C)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 10.63 20 with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 531.66. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.2 mM 9.4 mL 47.02 mL 94.05 mL
1 mM 1.88 mL 9.4 mL 18.81 mL
2 mM 0.94 mL 4.7 mL 9.4 mL
10 mM 0.19 mL 0.94 mL 1.88 mL

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References

References are publications that support the biological activity of the product.

Waszkowycz et al (2018) Cell-active small molecule inhibitors of the DNA-damage repair enzyme poly(ADP-ribose) glycohydrolase (PARG): discovery and optimization of orally bioavailable quinazolinedione sulfonamides. J.Med.Chem. 61 10767 PMID: 30403352


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Citations for PDD 00017272

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