BMN-673;LT-673 他拉唑帕利 Talazoparib
- 公司名稱 MedChemExpress LLC
- 品牌 MedChemExpress (MCE)
- 型號 BMN-673;LT-673
- 產(chǎn)地
- 廠商性質(zhì) 生產(chǎn)廠家
- 更新時間 2019/7/10 17:18:46
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抑制劑，調(diào)節(jié)劑，API，天然產(chǎn)物，各種類型化合物庫
| 供貨周期 | 現(xiàn)貨 | 規(guī)格 | 10 mM * 1 mL；2 mg；5 mg；10 mg；50 mg；100 m |
|---|---|---|---|
| 貨號 | HY-16106 | 應(yīng)用領(lǐng)域 | 生物產(chǎn)業(yè) |
Talazoparib
產(chǎn)品活性：Talazoparib (BMN-673) 是高效的 PARP1/2 抑制劑，Ki 值分別為 1.2 nM 和 0.87 nM。
研究領(lǐng)域：Cell Cycle/DNA Damage | Epigenetics
作用靶點(diǎn)：PARP
In Vitro: Talazoparib (BMN 673) demonstrates excellent potency, inhibiting PARP1 and PARP2 enzyme activity with Ki=1.2 and 0.87 nM, respectively. Talazoparib (BMN 673) exhibits selective antitumor cytotoxicity and elicits DNA repair biomarkers at much lower concentrations than earlier generation PARP1/2 inhibitors (such as Olaparib, Rucaparib, and Veliparib).
In Vivo: Talazoparib (BMN 673; 1 mg/kg, p.o.) is orally available, displaying favorable pharmacokinetic (PK) properties and remarkable antitumor efficacy in the BRCA1 mutant MX-1 breast cancer xenograft model following oral administration as a single-agent or in combination with chemotherapy agents such as temozolomide and cisplatin. Talazoparib (BMN 673) is readily orally bioavailable, with more than 40% absolute oral bioavailability in rats when dosed in carboxylmethyl cellulose. Oral administration of Talazoparib elicits remarkable antitumor activity, xenografted tumors that carry defects in DNA repair due to BRCA mutations or PTEN deficiency are profoundly sensitive to oral Talazoparib treatment at well-tolerated doses in mice.
相關(guān)產(chǎn)品：Drug Repurposing Compound Library | Clinical Compound Library | Clinical Compound Library Plus | Anti-Cancer Compound Library | Cell Cycle/DNA Damage Compound Library | Drug Repurposing Compound Library Plus | Epigenetics Compound Library | Bioactive Compound Library Plus | Olaparib | XAV-939 | Niraparib | Veliparib | Rucaparib phosphate | PJ34 hydrochloride | Pamiparib | Rucaparib Camsylate | G007-LK | Talazoparib tosylate | AZD-2461 | E7449 | NMS-P118 | AG14361 | Iniparib | JW 55 | A-966492 | AZ6102 | 3-Aminobenzamide | BGP-15 | ME0328 | MN-64 | NVP-TNKS656 | UPF 1069 | Dehydrocorydaline
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