[CAS NO. 1945950-21-9]  PDD 00017273

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PRODUCTS SPECIFICATIONS [1945950-21-9]

Catalog
HY-108360
Brand
MCE
CAS
1945950-21-9

DESCRIPTION [1945950-21-9]

Overview

MDL-
Molecular Weight514.62
Molecular FormulaC23H26N6O4S2
SMILESO=S(C1=CC2=C(N(CC3=CC(C)=NN3C)C(N(CC4=CN=C(C)S4)C2=O)=O)C=C1)(NC5(C)CC5)=O

For research use only. We do not sell to patients.


Summary

PDD 00017273 is a potent inhibitor of Poly(ADP-ribose) Glycohydrolase ( PARG ), with an IC 50 of 26 nM, and a K D of 1.45 nM [1] [2] .


IC50 & Target

IC50: 26 nM (PARG) [1]
KD: 1.45 nM (PARG) [1]


In Vitro

PDD 00017273 is a potent inhibitor of PARG, with an IC 50 of 26 nM, and a K D of 1.45 nM. PDD 00017273 (10 μM) does not inhibit five common Cytochrome P450 enzymes. PDD 00017273 (30 μM) modestly increasess phosphorylated H2AX (γH2AX) intensity, PDD 00017273 also decreases in NAD/H through PARG inhibition after DNA damage. PDD 00017273 suppresses the ZR-75-1 cells carring BRCA1 and BRCA2 wild type, and exhibits less potent activities against MDA-MB-436 cells carry the 5396 + 1G>A mutation in BRCA1 [1] . PDD 00017273 (0.3 μM) inhibits degradation of PAR polymers in MCF7 cells. PDD 00017273 (0.3 μM) also reduces the viability of BRCA1, BRCA2, PALB2, FAM175A, and BARD1 depleted cells. PDD 00017273 stalls replication forks and induces DNA damage that requires homologous recombination (HR) for repair [2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL ( 48.58 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 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
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.5 mg/mL (4.86 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.86 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.86 mM); Clear solution

* All of the co-solvents are available by MCE.