BMN-673 (Talazoparib)

製品コードS7048 バッチS704811

化学情報

	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	76 mg/mL (199.81 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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. Off-target molecular screening did not identify significant non-specific activity for this class of PARP inhibitors.
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.
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
A cancer persistent DNA repair circuit driven by MDM2, MDM4 (MDMX), and mutant p53 for recruitment of MDC1 and 53BP1 on chromatin [ Nucleic Acids Res, 2025, 53(13)gkaf627]	PubMed: 40626562
The inflammasome sensor NLRP3 interacts with REV7 to maintain genome integrity through homologous recombination [ Nucleic Acids Res, 2025, 53(12)gkaf554]	PubMed: 40613708
Combined MEK and PARP inhibition enhances radiation response in rectal cancer [ Cell Rep Med, 2025, 6(8):102284]	PubMed: 40782795
Targeting CDK12/13 Drives Mitotic Arrest to Overcome Resistance to KRASG12C Inhibitors [ Cancer Res, 2025, 10.1158/0008-5472.CAN-25-0450]	PubMed: 41165466
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

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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