>>

>>

抑制剂/激活剂

>>

凋亡与自噬

>>

BMN 673 他拉唑帕利; BMN-673; LT-673

Talazoparib (BMN 673, LT-673)是一种新型的PARP抑制剂，无细胞试验中对PARP1的IC50为0.57 nM。它也是有效的PARP-2抑制剂，但不抑制PARG，对PTEN突变型高度敏感。Phase 3。

货号：
TK0291
规格：

1mg

2mg

5mg
价格：
￥0.00

产品参数

CAS No.	1207456-01-6
生物活性	Talazoparib (BMN-673) is a highly potent, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with Kis of 1.2 nM and 0.87 nM, respectively. Talazoparib has antitumor activity.
分子式	C19H14F2N6O
分子量	380.35
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20℃ 3 years
溶解性数据	DMSO : 25 mg/mL (65.73 mM; Need ultrasonic)
体内研究	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). 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).
体外研究	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).
文献	暂无相关参考文献
纯度及产品资料	98%

推荐产品