Specifications
- Purity
- ≥98% (HPLC)
- Appearance
- Off-white to beige powder
- Identity
- 1H-NMR
Properties
- Solvents
- DMSO (20 mg/ml), DMF (10 mg/ml), ethanol (1mg/ml)
- Melting Point
- 198-209° C
Category: API's & Intermediates
Olaparib is a cell-permable potent inhibitor of PARP1 and PARP2 (IC50=5 and 1nM, respectively) but is less effective against the PARP tankyrase-1 (IC50=1.5µM). Some poly(ADP-ribose) polymerases (PARPs) assist in the repair of single-strand DNA nicks, an important step in base excision repair (BER), counteracting against DNA alkylating agents. Olaparib is a anticancer and chemotherapeutic agent (especially in cancers with BRCA mutations) that can be used in cells and in animals, alone or in combination therapy with alkylating agents, to block BER and increase cancer cell death.
Synonyms | AZD 2281, Ku-0059436, Lynparza, 1-(Cyclopropylcarbonyl)-4-[5-[(3,4-dihydro-4-oxo-1-phthalazinyl)methyl]-2-fluorobenzoyl]piperazine |
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Purity | ≥98% (HPLC) |
Appearance | Off-white to beige powder |
CAS-Number | 763113-22-0 |
Molecular Formula | C24H23FN4O3 |
Molecular Weight | 434.47 |
Identity | 1H-NMR |
Solvents | DMSO (20 mg/ml), DMF (10 mg/ml), ethanol (1mg/ml) |
Melting Point | 198-209° C |
Smiles | O=C(C1CC1)N2CCN(C(C3=C(F)C=CC(CC(C4=C5C=CC=C4)=NNC5=O)=C3)=O)CC2 |
InChi Key | FDLYAMZZIXQODN-UHFFFAOYSA-N |
Shipping | AMBIENT |
Short Term Storage | +4°C |
Long Term Storage | -20°C |
Handling Advice | Protect from light and moisture. |
Use / Stability | Stable for at least 2 years after receipt when stored at -20°C. |
Hazard statements | H301, H360D, H372, H412 |
GHS Symbol | GHS07 |
Signal word | Warning |
Transportation | Not dangerous goods |
References | (1) K.A. Menear, et al., J. Med. Chem. 51, 6581 (2008), (2) S. Rottenberg, et al., PNAS 105, 17079 (2008), (3) B.P. Rowe & P.M. Glazer, Breast Cancer Res. 12, 1 (2010), (4) Y. Yuan, et al., J. Hematol. Oncol. 4, 1 (2011), (5) R. Plummer, Breast Cancer Res. 13, 1 (2011), (6) M. Javle & N.J. Curtin, Ther. Adv. Med. Oncol. 3, 257 (2011), (7) D. Davar, et al., Curr. Med. Chem. 19, 3907 (2012), (8) C.C. Gunderson & K.N. Moore, Future Oncol. 11, 747 (2015), (9) F. De Felice, et al., Drug Des. Devel. Ther. 11, 547 (2017), (10) J. Stewart, et al., Expert Rev. Anticancer Ther. 18, 947 (2018) |
Quantity | 100 mg, 1 g, Bulk |