| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
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PDD00017273 is a novel, potent and selective poly (ADP ribose) glycohydrolase (PARG) inhibitor with an IC50 of 26 nM. PDD00017273 exhibits >350-fold selectivity for PARG over a panel of ion channels, enzymes and receptors, including PARP1 and ARH3.
| ln Vitro |
PDD 00017273 is a powerful PARG reagent with an IC50 of 26 nM and a KD of 1.45 nM. For five typical cytochrome P450 enzymes, PDD 00017273 (10 μM) does not inhibit. In addition to inhibiting NAD/H through PARG after DNA damage, PDD 00017273 (30 μM) increases the intensity of phosphorylated H2AX (γH2AX). When it comes to MDA-MB-436 cells labeled with 5396 + 1G>A in BRCA1, PDD 00017273 exhibits minimal activity, but it inhibits ZR-75-1 cells labeled with wild-type BRCA1 and BRCA2 [1]. The breakdown of PAR medium in MCF7 cells is inhibited by PDD 00017273 (0.3 μM). Additionally, BARD1, BRCA2, PALB2, FAM175A, and BRCA1 latency are decreased by PDD 00017273 (0.3 μM). Inducing DNA damage that must be repaired by homologous recombination (HR) and stopping replication forks are the effects of PDD 00017273 [2].
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| References |
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| Molecular Formula |
C23H26N6O4S2
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|---|---|
| Molecular Weight |
514.6203
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| CAS # |
1945950-21-9
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| Related CAS # |
1945950-21-9;
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| PubChem CID |
121398766
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| Appearance |
White to light yellow solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
35
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| Complexity |
954
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1C=CC2=C(C(N(CC3=CN=C(C)S3)C(N2CC2=CC(C)=NN2C)=O)=O)C=1)(NC1(C)CC1)(=O)=O
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| InChi Key |
IFWUBRBMMNTBRZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H26N6O4S2/c1-14-9-16(27(4)25-14)12-28-20-6-5-18(35(32,33)26-23(3)7-8-23)10-19(20)21(30)29(22(28)31)13-17-11-24-15(2)34-17/h5-6,9-11,26H,7-8,12-13H2,1-4H3
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| Chemical Name |
1-[(1,3-Dimethyl-1H-pyrazol-5-yl)methyl]-1,2,3,4-tetrahydro-N-(1-methylcyclopropyl)-3-[(2-methyl-5-thiazolyl)methyl]-2,4-dioxo-6-quinazolinesulfonamide
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| Synonyms |
PDD-00017273 PDD 00017273 PDD00017273 PDD-17273 PDD 17273 PDD 17273
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~48.58 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.86 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.86 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.86 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9432 mL | 9.7159 mL | 19.4318 mL | |
| 5 mM | 0.3886 mL | 1.9432 mL | 3.8864 mL | |
| 10 mM | 0.1943 mL | 0.9716 mL | 1.9432 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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