| 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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| 100mg |
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Saruparib (AZD 5305; AZD-5305; AZD5305) is a novel, potent, selective and orally bioactive PARP [Poly(ADP-ribose)polymerase-1] inhibitor with anticancer activity. Its IC50 values for PARP1/2 inhibition are 3 nM and 1400 nM, respectively.
| Targets |
PARP1 ( IC50 = 3 nM ); PARP2 ( IC50 = 1400 nM )
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| ln Vitro |
AZD5305 has excellent pharmacokinetics in preclinical species, good secondary pharmacology, good physicochemical properties, and is a highly selective inhibitor for PARP1 over other PARP family members. In vitro, AZD5305 lessens the anti-proliferation effects on human bone marrow progenitor cells.
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| ln Vivo |
AZD5305 exhibits excellent in vivo efficacy as a potent and selective PARP1 inhibitor and PARP1-DNA trapper in a BRCA mutant HBCx-17 PDX model.[2]
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| Cell Assay |
BRCA2 and DLD-1(-/-) Using a Multidrop Combi, 40 μL of DLD-1 cells per well are seeded into 384-well plates at a density of 5000 cells/mL and 2.5 × 104 cells/mL, respectively, in complete media. The plates are then incubated for an overnight period at 37 °C with 5% CO2. Day 0 plate was incubated for more than three hours at room temperature (RT) after sytox green (5 μL, 2 μM) and saponin (10 μL, 0.25% stock) were added using a Multidrop Combi. The plate was then sealed with a black adhesive lid. Cell Insight Focused with a 4× objective is used to image cells. Using an Echo 555, AZD5305 is added, and the mixture is then incubated for seven days at 37 °C with 5% CO2. Day 8: Plates are filled with sytox green (5 μL, 2 μM) and saponin (10 μL, 0.25% stock). A black adhesive lid is used to seal the plate, and it is incubated for more than three hours at room temperature. On a 4× Objective Cell Insight, every cell is read.
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| References |
| Molecular Formula |
C22H26N6O2
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|---|---|
| Molecular Weight |
406.49
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| Exact Mass |
406.21
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| Elemental Analysis |
C, 65.01; H, 6.45; N, 20.68; O, 7.87
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| CAS # |
2589531-76-8
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| Appearance |
Solid powder
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| SMILES |
CCC1=CC2=C(C=C(C=N2)CN3CCN(CC3)C4=CN=C(C=C4)C(=O)NC)NC1=O
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| InChi Key |
WQAVGRAETZEADU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H26N6O2/c1-3-16-11-19-20(26-21(16)29)10-15(12-24-19)14-27-6-8-28(9-7-27)17-4-5-18(25-13-17)22(30)23-2/h4-5,10-13H,3,6-9,14H2,1-2H3,(H,23,30)(H,26,29)
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| Chemical Name |
5-[4-[(7-ethyl-6-oxo-5H-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl]-N-methylpyridine-2-carboxamide
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| Synonyms |
AZD-5305; AZD5305; AZD 5305
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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: 12.5~20 mg/mL (30.8~49.2 mM)
Ethanol: 2 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.56 mg/mL (1.38 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 5.6 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: ≥ 0.56 mg/mL (1.38 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 5.6 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: ≥ 0.56 mg/mL (1.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5%DMSO+ 40%PEG300+ 5%Tween 80+ 50%ddH2O: 0.8mg/ml (1.97mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4601 mL | 12.3004 mL | 24.6009 mL | |
| 5 mM | 0.4920 mL | 2.4601 mL | 4.9202 mL | |
| 10 mM | 0.2460 mL | 1.2300 mL | 2.4601 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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