商品编号


6060



品牌


Tocris



公司


Bio-Techne Corporation



公司分类


Polymerases



Size

10 mg

商品信息

Description:
Potent PARP inhibitor; orally bioavailable

Chemical Name:
4-[[4-Fluoro-3-[(4-methoxy-1-piperidinyl)carbonyl]phenyl]methyl]-1(2
H
)-phthalazinone

Purity:
≥98% (HPLC)


BIOLOG
ical Activity Technical Data Solubility Calculators Datasheets References


BIOLOG
ical Activity

Potent PARP inhibitor (IC
50
values are 2, 5 and 200 nM for PARP2, PARP1 and PARP3, respectively). Exhibits anticancer effects in
BRCA1
mutant, but not wild-type breast cancer cell lines
in vitro
. Inhibits growth of olaparib-resistant mammary tumors in a mouse model and is a poor substrate for the P-gp transporter. Orally bioavailable.



Technical Data



M. Wt

395.43



Formula

C
22
H
22
FN
3
O
3




Storage

Store at -20°C



Purity

≥98% (HPLC)



CAS Number

1174043-16-3



PubChem ID

44199317



InChI Key

HYNBNUYQTQIHJK-UHFFFAOYSA-N



Smiles

COC1CCN(C(C2=C(C=CC(CC3=NNC(C4=CC=CC=C34)=O)=C2)F)=O)CC1



The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All
Tocris
products are intended for laboratory research use only.



Solubility Data




Solvent

Max Conc. mg/mL

Max Conc. mM



Solubility



DMSO

39.54

100



ethanol

39.54

100





Preparing Stock Solutions

The following data is based on the
product
molecular weight
395.43
. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.



Concentration / Solvent Volume / Mass

1 mg

5 mg

10 mg



1 mM

2.53 mL

12.64 mL

25.29 mL



5 mM

0.51 mL

2.53 mL

5.06 mL



10 mM

0.25 mL

1.26 mL

2.53 mL



50 mM

0.05 mL

0.25 mL

0.51 mL






Molarity Calculator






Molarity Calculator

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Reconstitution Calculator






Reconstitution Calculator



The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.



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Dilution Calculator






Dilution Calculator

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Product Datasheets


Certificate of Analysis / Product Datasheet


Safety Datasheet

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References

References are publications that support the products'
BIOLOG
ical activity.


Oplustil O'Connor

et al
(2016) The PARP inhibitor AZD2461 provides insights into the role of PARP3 inhibition for both synthetic lethality and toler
ABI
lity with chemotherapy in preclinical models. Cancer Res.
76
6084 PMID: 27550455


Jaspers

et al
(2013) Loss of 53BP1 causes PARP inhibitor resistance in Brca1-mutated mouse mammary tumors. Cancer Discov.
3
68 PMID: 23103855




Keywords: AZD 2461, supplier, AZD2461, potent, PARP, inhibitors, inhibits, poly, (ADP-ribose), polymerases, orally, bioavailable, chemotherapeutics, Poly(ADP-ribose), Polymerase,
Tocris
Bioscience