Talazoparib (BMN-673)

製品コードS7048 バッチS704813

印刷

化学情報

Chemical Structure Synonyms LT-673 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

 

C19H14F2N6O
 
分子量 380.35 CAS No. 1207456-01-6
Solubility (25°C)* 体外 DMSO (warmed with 50ºC water bath) 19 mg/mL (49.95 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 タラゾパリブ (Talazoparib (BMN 673、LT-673)) は、新規 PARP 阻害剤 (無細胞アッセイで IC50 = 0.57 nM) です。 また PARP-2 の強力な阻害剤でもありますが、PARG を阻害せず PTEN 変異に非常に敏感です。 臨床フェーズ 3。
in vitro

BMN-673 selectively binds to PARP and prevents PARP-mediated DNA repair of single strand DNA breaks via the base-excision repair pathway. This enhances the accumulation of DNA strand breaks, promotes genomic instability and eventually leads to apoptosis. BMN 673 selectively kills cancer cells with BRCA-1 or BRCA-2 mutations. BMN 673 demonstrates single-agent cytotoxicityin BRCA-1 mutant (MX-1, IC50 = 0.3 nM) and BRCA-2 mutant cells (Capan-1, IC50 = 5 nM). In contrast, in MRC-5 normal human fibroblastand other tumor cell lines with wild-type BRCA-1 and BRCA-2 genes, IC50 of BMN 673 ranges between 90 nM and 1.9 μM. [1]

Off-target molecular screening did not identify significant non-specific activity for this class of PARP inhibitors. [2]
in vivo

In rat pharmacokinetic studies, BMN 673 displays >50% oralbioavailability and pharmacokinetic properties that enable singledaily dosing. In MX-1 xenograft tumor model studies, daily oral dosingof BMN 673 significantly enhances the antitumor effects ofcytotoxic therapies in a dose-dependent manner. [2]
特徴 Most potent and selective PARPi reported thus far.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 MDA-MB-436 cells
濃度 10 uM
反応時間 7 days
実験の流れ

Cells were treated with increasing doses of talazoparib for 7 days and subjected to cell viability assays to derive IC50 values.
動物実験 動物モデル MX-1 model (BRCA-1 deficient)
投薬量 0.33 mg/kg/day, once daily
投与方法 Oral

参考

  • http://www.selleckchem.com/products/bmn-673.html
  • http://cancerres.aacrjournals.org/cgi/content/meeting_abstract/70/8_MeetingAbstracts/3514
  • https://pubmed.ncbi.nlm.nih.gov/31015319/

カスタマーフィードバック

, , Clin Cancer Res, 2017, 23(13):3405-3415

Data from [Data independently produced by , , Nature, 2018, 559(7713):285-289]

Data from [Data independently produced by , , Clin Cancer Res, 2017, 23(14):3711-3720]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Jab1 regulates HRR mRNA stability to modulate PARP inhibitor sensitivity in triple-negative breast cancer [ Mol Cancer, 2025, 24(1):217] PubMed: 40819058
EXO1 as a therapeutic target for Fanconi Anaemia, ZRSR2 and BRCA1-A complex deficient cancers [ Nat Commun, 2025, 16(1):8476] PubMed: 41006228
Autocrine interferon poisoning mediates ADAR1-dependent synthetic lethality in BRCA1/2-mutant cancers [ Nat Commun, 2025, 16(1):6972] PubMed: 40730818
Combined MEK and PARP inhibition enhances radiation response in rectal cancer [ Cell Rep Med, 2025, 6(8):102284] PubMed: 40782795
PARP inhibitor-induced anti-tumour chemokine response is suppressed by dipeptidyl peptidase 4 (DPP4) in ovarian cancer [ Br J Cancer, 2025, 10.1038/s41416-025-03076-4] PubMed: 40579444
BCL2 drives castration resistance in castration-sensitive prostate cancer by orchestrating reciprocal crosstalk between oncogenic pathways [ Cell Rep, 2025, 44(6):115779] PubMed: 40448998
Low dose DNA methyltransferase inhibitors potentiate PARP inhibitors in homologous recombination repair deficient tumors [ Breast Cancer Res, 2025, 27(1):8] PubMed: 39819384
PARP inhibitors elicit distinct transcriptional programs in homologous recombination competent castration-resistant prostate cancer [ Mol Oncol, 2025, 10.1002/1878-0261.70098] PubMed: 40915979
Homologous Repair-Deficient Pancreatic Cancer: Refined Targeting of DNA Damage Response is an Effective Therapeutic Strategy [ United Eur Gastroent, 2025, 13(7):1328-1342] PubMed: 40823818
Steroid-Modulated Transcription Synergistically Forms DNA Double-Strand Breaks With Topoisomerase II Inhibitor [ Cancer Sci, 2025, 10.1111/cas.70081] PubMed: 40231641

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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