货号:A570059 同义名: BMN-673;LT-673
Talazoparib (BMN-673) 是一种高效、口服活性的PARP1/2抑制剂,对PARP1和PARP2的Ki值分别为1.2 nM和0.87 nM。它具有抗肿瘤活性。
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产品名称 | PARP ↓ ↑ | PARP1 ↓ ↑ | PARP2 ↓ ↑ | PARP3 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
PJ34 HCl |
++
PARP, EC50: 20 nM |
99%+ | |||||||||||||||||
Rucaparib phosphate |
++++
PARP, Ki: 1.4 nM |
99%+ | |||||||||||||||||
3-Aminobenzamide |
++
PARP, IC50: <50 nM |
98% | |||||||||||||||||
AZD-2461 | ✔ | 99%+ | |||||||||||||||||
BGP-15 | ✔ | 99%+ | |||||||||||||||||
NU1025 |
+
PARP, IC50: 400 nM |
97% | |||||||||||||||||
Benzamide |
+
PARP, IC50: 3.3 μM |
98% | |||||||||||||||||
Picolinamide |
+
PARP, IC50: 95 μM |
98% | |||||||||||||||||
AG14361 |
+++
PARP1, Ki: <5 nM |
98+% | |||||||||||||||||
Iniparib | ✔ | 98% | |||||||||||||||||
Talazoparib |
++++
PARP1, IC50: 0.57 nM |
99%+ | |||||||||||||||||
NMS-P118 |
++
PARP1, Kd: 0.009 μM |
98+% | |||||||||||||||||
UPF 1069 |
+
PARP1, IC50: 8.0 μM |
++
PARP2, IC50: 0.3 μM |
98% | ||||||||||||||||
A-966492 |
++++
PARP1, Ki: 1 nM PARP1, EC50: 1 nM |
+++
PARP2, Ki: 1.5 nM |
99%+ | ||||||||||||||||
Veliparib |
++
PARP1, Ki: 5.2 nM |
+++
PARP2, Ki: 2.9 nM |
98% | ||||||||||||||||
Niraparib tosylate |
+++
PARP1, IC50: 3.8 nM |
+++
PARP2, IC50: 2.1 nM |
99%+ | ||||||||||||||||
Stenoparib |
++++
PARP1, IC50: 1 nM |
++++
PARP2, IC50: 1.2 nM |
98% | ||||||||||||||||
Olaparib |
+++
PARP1, IC50: 5 nM |
++++
PARP2, IC50: 1 nM |
98% | ||||||||||||||||
Niraparib |
+++
PARP1, IC50: 3.8 nM |
+++
PARP2, IC50: 2.1 nM |
98% | ||||||||||||||||
ME0328 |
+
PARP1, IC50: 6.3 μM |
+
PARP3, IC50: 0.89 μM |
99%+ | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | PARP1, also called as Poly(ADP-ribose) polymerase, is involved in the signaling of DNA damage. It can recognize and bind DNA single or double-strand breaks, thus possessing various cellular function, including regulation of apoptosis and chromosome stability, gene amplification and transcription, as well as cell division and differentiation. PARP-2 is the closest homolog of PARP1 (~62% similarity in catalytic domain) and compensates for PARP-1 activity in DNA single-strand break. BMN 673 is a potent PARP1/2 inhibitor with IC50 value of 0.57nM for PARP1 (measured by PARP1 enzyme activity). BMN673 showed EC50 value of 2.5nM for inhibition of cellular PAR synthesis in LoVo cells, IC50 value of 5nM for single-agent cytotoxicity of Capan-1 cell survival reduction and GI50 value of 3nM for Temozolomide potentiation assay in LoVo cells. BMN 673 selectivity inhibited BRCA-deficient cells and delivered a therapeutic window between BRCA-proficient and –deficient models at much lower concentrations compared with the other PARP inhibitor, veliparib, rucaparib and olaparib. BMN 673 possessed good pharmacodynamics, as a single oral administration of 1 mg/kg BMN 673 caused drastically decreased intratumoral PAR levels at 2 and 8 hours following drug administration with partial recovery observed at 24 hours after dosing. Oral administration of BMN 673 at dose of 0.33mg/kg, daily, for 28 days caused significant growth inhibition of MX-1 xenografts in mice[1]. BMN 673 showed ~100-fold more potent at trapping PARP-DNA complexes and more cytotoxic as single agent than olaparib[2]. |
作用机制 | BMN 673 is anchored to the nicotinamide-binding pocket of PARP and extends the binding interactions towards the outer edges of the pocket, which exhibit the least sequence homology among PARP enzymes.[3] |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
BR5FVB1-Akt | 0.1-100 nM | Growth Inhibition Assay | 24/48/72 h | inhibits cell proliferation dose dependently | 26047697 |
BR5FVB1-Akt | 0.1-100 nM | Apoptosis Assay | 72 h | induces apoptosis | 26047697 |
BT-12 | Growth Inhibition Assay | IC50> 1,000 nM | 25263539 | ||
Capan-1 | Growth Inhibition Assay | IC50=16.0 ± 5.4 µM | 25864590 | ||
Dose | Nude Mice: o.1 mg/kg, 0.33 mg/kg[1] (p.o.) |
Administration | p.o. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.63mL 0.53mL 0.26mL |
13.15mL 2.63mL 1.31mL |
26.29mL 5.26mL 2.63mL |
CAS号 | 1207456-01-6 |
分子式 | C19H14F2N6O |
分子量 | 380.35 |
别名 | BMN-673;LT-673 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
溶解度 |
DMSO: 25 mg/mL(65.73 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |
IP 2% DMSO+2% Tween80+40% PEG300+water 2 mg/mL clear PO 0.5% CMC-Na 45 mg/mL suspension |