Olaparib-d4-1
Based on 1 Customer Validation
Olaparib-d4-1 (AZD2281-d4-1) is the deuterium labeled Olaparib (HY-10162). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator.
For research use only. We do not sell to patients.
- Purity: 98.82%
- CAS No.: 2143107-55-3
- Formula: C24H19D4FN4O3
- Molecular Weight:438.49
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS No. 2143107-55-3
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Unlabeled Cas 763113-22-0
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Appearance Solid
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Molecular Weight 438.49
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Formula C24H19D4FN4O3
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Color White to off-white
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SMILES
O=C(N1CCN(CC1)C(C2=C(C=CC(CC(C3=C4C=CC=C3)=NNC4=O)=C2)F)=O)C5C([2H])(C5([2H])[2H])[2H]
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Synonyms
AZD2281-d4-1; KU0059436-d4-1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (228.06 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
DMF : 50 mg/mL (114.03 mM; Need ultrasonic)
Ethanol : 3.12 mg/mL (7.12 mM; ultrasonic and warming and heat to 60°C)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [Content Brief]
[2]. Menear KA, et al. 4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1. J Med Chem. 2008 Oct 23;51(20):6581-91 [Content Brief]
[3]. Senra JM, et al. Inhibition of PARP-1 by olaparib (AZD2281) increases the radiosensitivity of a lung tumor xenograft.Mol Cancer Ther. 2011 Oct;10(10):1949-58. [Content Brief]
[4]. Yasukawa M, et al. Synergetic Effects of PARP Inhibitor AZD2281 in Oral Squamous Cell Carcinoma in Vitro and in Vivo. Int J Mol Sci. 2016 Feb 24;17(3):272. [Content Brief]
[5]. Bian X, et al. PTEN deficiency sensitizes endometrioid endometrial cancer to compound PARP-PI3K inhibition but not PARP inhibition as monotherapy. Oncogene. 2018 Jan 18;37(3):341-351. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| Ethanol / DMF / DMSO | 1 mM | 2.2806 mL | 11.4028 mL | 22.8055 mL | 57.0138 mL |
| 5 mM | 0.4561 mL | 2.2806 mL | 4.5611 mL | 11.4028 mL | |
| DMF / DMSO | 10 mM | 0.2281 mL | 1.1403 mL | 2.2806 mL | 5.7014 mL |
| 15 mM | 0.1520 mL | 0.7602 mL | 1.5204 mL | 3.8009 mL | |
| 20 mM | 0.1140 mL | 0.5701 mL | 1.1403 mL | 2.8507 mL | |
| 25 mM | 0.0912 mL | 0.4561 mL | 0.9122 mL | 2.2806 mL | |
| 30 mM | 0.0760 mL | 0.3801 mL | 0.7602 mL | 1.9005 mL | |
| 40 mM | 0.0570 mL | 0.2851 mL | 0.5701 mL | 1.4253 mL | |
| 50 mM | 0.0456 mL | 0.2281 mL | 0.4561 mL | 1.1403 mL | |
| 60 mM | 0.0380 mL | 0.1900 mL | 0.3801 mL | 0.9502 mL | |
| 80 mM | 0.0285 mL | 0.1425 mL | 0.2851 mL | 0.7127 mL | |
| 100 mM | 0.0228 mL | 0.1140 mL | 0.2281 mL | 0.5701 mL |