Talazoparib free base · Synonyms: BMN-673 | LT-673

Talazoparib is a highly potent PARP1/2 inhibitor.

For research use only. Not for human or veterinary use.

Target PARP

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

Talazoparib structure

CAS No.: 1207456-01-6

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 410.00	BP-02324-250mg	In stock	Get quote
500 mg	USD 660.00	BP-02324-500mg	In stock	Get quote
1 g	USD 1,050.00	BP-02324-1g	In stock	Get quote
2 g	USD 1,680.00	BP-02324-2g	In stock	Get quote
3 g	USD 2,016.00	BP-02324-3g	In stock	Get quote
5 g	USD 2,680.00	BP-02324-5g	In stock	Get quote
10 g	USD 4,300.00	BP-02324-10g	In stock	Get quote

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Description

Talazoparib (BMN-673) is a highly potent PARP1/2 inhibitor with Kis of 1.2 nM and 0.87 nM respectively.

Biological activity

In Vitro Talazoparib shows an EC50 of 2.51 nM in cellular PARylation assay. Talazoparib shows EC50s of 0.3 nM, 5 nM and 0.31 for MX-1 cells (BRCA1 mutant), Capan-1 cells (BRCA2 mutant) and MRC-5 cells (normal). In Vivo Talazoparib (0.33 mg/kg; i.g.; once daily; for 28 days) exhibits antitumor activity against BRCA1 mutant breast cancer model in mice. Talazoparib exhibits moderate oral bioavailability (rat 56%) and Cmax (rat 7948 ng/mL) following oral administration (rat 10 mg/kg)[1]. Talazoparib exhibits the terminal elimination half-life (rat 2.25 h) due to plasma clearance (2 mL/min/kg) following intravenous administration (rat 5 mg/kg).

Identifiers

SMILES: CN1N=CN=C1[C@@H]1[C@H](N=C2C=C(F)C=C3C(=O)NNC1=C23)C1=CC=C(F)C=C1
InChIKey: IUEWAGVJRJORLA-HZPDHXFCSA-N

Specifications

MW (average): 380.3509
Formula: C₁₉H₁₄F₂N₆O
CAS No.: 1207456-01-6
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Wang B, et al. Discovery and Characterization of (8S,9R)-5-Fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-2,7,8,9-tetrahydro-3H-pyrido[4,3,2-de]phthalazin-3-one (BMN 673, Talazoparib), a Novel, Highly Potent, and Orally Efficacious Poly(ADP-ribose) Polymerase-1/2 Inhibitor, as an Anticancer Agent. J Med Chem. 2016 Jan 14;59(1):335-57.

[2]. Shen Y, et al. BMN 673, a novel and highly potent PARP1/2 inhibitor for the treatment of human cancers with DNA repair deficiency.Clin Cancer Res. 2013 Sep 15;19(18):5003-15.

Same target

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Same research area

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