1. Cell Cycle/DNA Damage Epigenetics
  2. PARP
  3. (rac)-Talazoparib

(rac)-Talazoparib  (Synonyms: (rac)-BMN-673; (rac)-LT-673)

Art. -Nr.: HY-14687
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(rac)-Talazoparib ((rac)-BMN-673) (Compound 47) is the orally active inhibitor for PARP1/2 with Ki of 1.2 nM and 0.87 nM. (rac)-Talazoparib inhibits cellular PARylation with an EC50 of 2.51 nM. (rac)-Talazoparib causes the accumulation of DNA damage, inhibits proliferation of BRCA1/2-mutated MX-1 cell and Capan-1 cell with IC50 of 0.3 nM and 5 nM. (rac)-Talazoparib exhibits antitumor efficacy in mouse models.

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(rac)-Talazoparib

(rac)-Talazoparib Chemische Struktur

CAS. Nr. : 1207454-56-5

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Beschreibung

(rac)-Talazoparib ((rac)-BMN-673) (Compound 47) is the orally active inhibitor for PARP1/2 with Ki of 1.2 nM and 0.87 nM. (rac)-Talazoparib inhibits cellular PARylation with an EC50 of 2.51 nM. (rac)-Talazoparib causes the accumulation of DNA damage, inhibits proliferation of BRCA1/2-mutated MX-1 cell and Capan-1 cell with IC50 of 0.3 nM and 5 nM. (rac)-Talazoparib exhibits antitumor efficacy in mouse models[1].

IC50 & Target

PARP2

0.87 nM (Ki)

PARP1

1.2 nM (Ki)

Cellular Effect
Cell Line Type Value Description References
CAPAN-1 EC50
0.008 μM
Compound: 47
Cytotoxicity against BRCA2-deficient human Capan1 cells
Cytotoxicity against BRCA2-deficient human Capan1 cells
[PMID: 26652717]
LoVo EC50
5.48 nM
Compound: 47
Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay
Inhibition of PARP in human LoVo cells assessed as inhibition of poly(ADP)-ribose polymerization for 30 mins by fluorescence assay
[PMID: 26652717]
LoVo GI50
19 μM
Compound: 47
Potentiation of temozolomide-induced cytotoxicity in human LoVo cells assessed as temozolomide GI50 at 0.4 uM after 5 days by Celltiter-Glo assay
Potentiation of temozolomide-induced cytotoxicity in human LoVo cells assessed as temozolomide GI50 at 0.4 uM after 5 days by Celltiter-Glo assay
[PMID: 26652717]
Molekulargewicht

380.35

Formel

C19H14F2N6O

CAS. Nr.
SMILES

O=C1NN=C2C(C(NC3=CC(F)=CC1=C32)C4=CC=C(C=C4)F)C5=NC=NN5C

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Produktname:
(rac)-Talazoparib
Art. -Nr.:
HY-14687
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