BMN-673 8R,9S

BMN-673 8R,9S ((8R,9S)-BMN-673) 是 Talazoparib 的对映异构体。 BMN-673 8R,9S 是一种 PARP1 抑制剂，IC50 为 144 nM。

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库存: 现货

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5mg

￥1712.00

1370.00

- +
10mg

￥2275.00

1820.00

- +
50mg

￥5375.00

4300.00

- +
200mg

￥13475.00

10780.00

- +

已选 0 种 0 瓶

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货号: ajci6082
CAS: 1207456-00-5
别名: 他拉唑帕利 (8R,9S); (8R,9S)-BMN-673; (8R,9S)-LT-673
分子式: C19H14F2N6O
分子量: 380.35
纯度: >98%
溶解度: ≥ 38 mg/mL in DMSO with gentle warming, ≥ 22.55 mg/mL in EtOH with gentle warming
储存: Store at -20°C
库存: 现货

Background

PARP1/2 inhibitors are a class of anticancer agents that target tumor-specific defects in DNA repair. BMN 673 is a highly potent PARP1/2 inhibitor.
In vitro: BMN 673 is a potent PARP1/2 inhibitor, but it does not inhibit other enzymes that we have tested. BMN673 exhibits selective antitumor cytotoxicity and elicits DNA repair biomarkers at much lower concentrations than earlier generation PARP1/2 inhibitors. BMN 673 targeted tumor cells with BRCA1, BRCA2, or PTEN gene defects selectively with 20- to more than 200-fold greater potency than existing PARP1/2 inhibitors in vitro [1].
In vivo: BMN 673 is readily orally bioavailable, with more than 40% absolute oral bioavailability in rats when dosed in CMC. Orally BMN 673 elicited remarkable antitumor activity in mice; xenografted tumors that carry defects in DNA repair due to BRCA mutations or PTEN deficiency were profoundly sensitive to oral BMN 673 treatment at well-tolerated doses. Synergistic antitumor effects were also found when BMN 673 was combined with temozolomide, SN38, or platinum drugs [1].
Clinical trial: Pharmacokinetics (PK), pharmacodynamics (PD), safety and anti-tumor activity of BMN 673 were evaluated in a 2-stage dose-escalation study with 3-6 patients (pts)/dose level. Results showed BMN 673 was well tolerated with impressive anti-tumor activity in pts with BRCA mut with a single agent recommended Phase II trial dose of 1000 μg/d due to dose-limiting thrombocytopenia.
Reference:
[1] Shen Y, Rehman FL, Feng Y, Boshuizen J, Bajrami I, Elliott R, Wang B, Lord CJ, Post LE, Ashworth A. BMN 673, a novel and highly potent PARP1/2 inhibitor for the treatment of human cancers with DNA repair deficiency. Clin Cancer Res. 2013;19(18):5003-15.