Olaparib

CAS No. 763113-22-0

Olaparib( AZD2281 | KU-0059436 | KU0059436 | | AZD 2281 )

Catalog No. M15896 CAS No. 763113-22-0

A potent, specific, and orally active PARP inhibitor with IC50 of 5 and 1 nM for PARP1 and PARP2, respectively.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 28 In Stock
10MG 43 In Stock
50MG 61 In Stock
100MG 82 In Stock
200MG 108 In Stock
500MG 161 In Stock
1G 222 In Stock

Biological Information

  • Product Name
    Olaparib
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, specific, and orally active PARP inhibitor with IC50 of 5 and 1 nM for PARP1 and PARP2, respectively.
  • Description
    A potent, specific, and orally active PARP inhibitor with IC50 of 5 and 1 nM for PARP1 and PARP2, respectively; displays 300-fold selectivity over tankyrase (TNKS-1 IC50=1.5 uM); shows standalone activity against BRCA1-deficient breast cancer cell lines; regresses autochthonous Brca2/p53-mutant mammary tumors in vivo and delays tumor relapse in combination with carboplatin.Ovarian Cancer Approved(In Vitro):Olaparib (AZD2281) is a single digit nanomolar inhibitor of both PARP-1 and PARP-2 that shows standalone activity against BRCA1-deficient breast cancer cell lines. Olaparib is applied to SW620 cell lysates, and identified the IC50 for PARP-1 inhibition to be around 6 nM and the total ablation of PARP-1 activity to be at concentrations of 30?100 nM.(In Vivo):Animals bearing SW620 xenografted tumors are treated with Olaparib (10 mg/kg, p.o.) in combination with NSC 362856 (TMZ) (50 mg/kg, p.o.) once daily for 5 consecutive days, after which the tumors are left to grow out. Olaparib increases vascular perfusion in Calu-6 tumors established in a DWC model. Administration of olaparib(50 mg/kg, p.o.) as a single agent (top panel) or in combination with radiation (bottom panel) results in an increase in fluorescence intensity in the Calu-6 tumors.
  • In Vitro
    ——
  • In Vivo
    ——
  • Synonyms
    AZD2281 | KU-0059436 | KU0059436 | | AZD 2281
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    PARP
  • Recptor
    PARP1|PARP2
  • Research Area
    Cancer
  • Indication
    Ovarian Cancer

Chemical Information

  • CAS Number
    763113-22-0
  • Formula Weight
    434.4628
  • Molecular Formula
    C24H23FN4O3
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: 29 mg/mL
  • SMILES
    O=C1NN=C(CC2=CC=C(F)C(C(N3CCN(C(C4CC4)=O)CC3)=O)=C2)C5=C1C=CC=C5
  • Chemical Name
    1(2H)-Phthalazinone, 4-[[3-[[4-(cyclopropylcarbonyl)-1-piperazinyl]carbonyl]-4-fluorophenyl]methyl]-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Menear KA, et al. J Med Chem. 2008 Oct 23;51(20):6581-91. 2. Evers B, et al. Clin Cancer Res. 2008 Jun 15;14(12):3916-25. 3. Rottenberg S, et al. Proc Natl Acad Sci U S A. 2008 Nov 4;105(44):17079-84. 4. Hay T, et al. Cancer Res. 2009 May 1;69(9):3850-5.
molnova catalog
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