Size | Price | Stock | Qty |
---|---|---|---|
1mg |
|
||
5mg |
|
||
10mg |
|
||
Other Sizes |
|
ln Vitro |
Regardless of the status of homologous recombination repair (HRR), AZD-9574 inhibits the enzymatic activity of PARP1 in all tested cell lines, with an IC50 ranging between 0.3-2 nM [1]. In homogenous cell lines, higher efficacy and effects were shown on HRR-deficient (HRD+) models (DLD1 BRCA2-/-, SKOV-3 BRCA2-/-, and SKOV-3 PALB2-/-). Compared to BRCA2wt cells, which had an IC50 >40 μM, BRCA2-/-DLD1 cells had an IC50 of 1.38 nM[1].
|
---|---|
ln Vivo |
In an intracranial xenograft model of breast cancer brain metastases, AZD-9574 (3 mg/kg) displayed persistent growth suppression, greatly extending tumor-bearing tumor survival [1].
|
References |
[1]. Hybrid meeting divulges structures of drug candidates
[2]. 1.Kunzah Jamal, et al. Abstract 2609: AZD9574 is a novel, brain penetrant PARP-1 selective inhibitor with activity in an orthotopic, intracranial xenograft model with aberrant DNA repair. Cancer Res (2022) 82 (12_Supplement): 2609. |
Molecular Formula |
C21H22F2N6O2
|
---|---|
Molecular Weight |
428.44
|
Exact Mass |
428.18
|
Elemental Analysis |
C, 58.87; H, 5.18; F, 8.87; N, 19.62; O, 7.47
|
CAS # |
2756333-39-6
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
CC1=NC2=C(C(=C(C=C2)CN3CCN(CC3)C4=C(N=C(C=C4)C(=O)NC)F)F)NC1=O
|
Synonyms |
AZD9574; AZD-9574; AZD 9574;
|
HS Tariff Code |
2934.99.9001
|
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)
|
Solubility (In Vitro) |
DMSO : ~22.22 mg/mL (~51.86 mM)
DMSO : ~8.33 mg/mL (~19.44 mM) |
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.22 mg/mL (5.18 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 22.2 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: ≥ 2.22 mg/mL (5.18 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 22.2 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: ≥ 2.22 mg/mL (5.18 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 | 2.3340 mL | 11.6702 mL | 23.3405 mL | |
5 mM | 0.4668 mL | 2.3340 mL | 4.6681 mL | |
10 mM | 0.2334 mL | 1.1670 mL | 2.3340 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.