规格

价格

库存

数量

1 mg

¥ 303

现货

5 mg

¥ 675

现货

10 mg

¥ 1,190

现货

25 mg

¥ 2,670

现货

50 mg

¥ 4,130

现货

100 mg

¥ 5,890

现货

200 mg

¥ 8,020

现货

1 mL x 10 mM (in DMSO)

¥ 712

现货

生物活性

产品描述

Pirtobrutinib (LOXO-305) is an advanced BTK inhibitor that displays high selectivity and operates through a non-covalent mechanism. This compound effectively inhibits various BTK C481 substitution mutations, leading to tumor regression in BTK-dependent lymphoma tumors in mouse xenograft models. Furthermore, Pirtobrutinib exhibits remarkable selectivity for BTK, with more than a 300-fold difference compared to 370 other kinases tested. Notably, at a concentration of 1 μM, Pirtobrutinib demonstrates no significant inhibition of non-kinase off-targets.

体外活性

Pirtobrutinib以nM级的效力强效抑制了野生型BTK及BTK C481S介导的激酶活性。Pirtobrutinib对WT BTK (Y223) 自磷酸化显示出强烈的抑制作用，其IC50为3.68 nM。同样，Pirtobrutinib对BTK C481S Y223、C481T Y223以及C481R Y223的自磷酸化也表现出显著抑制，其IC50分别为8.45、7.23和11.73 nM[1]。

化学信息

分子量	479.43
分子式	C₂₂H₂₁F₄N₅O₃
CAS No.	2101700-15-4
Smiles	COc1ccc(F)cc1C(=O)NCc1ccc(cc1)-c1nn([C@@H](C)C(F)(F)F)c(N)c1C(N)=O
密度	1.44 g/cm3 (Predicted)

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 250 mg/mL (521.45 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.17 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0858 mL	10.4291 mL	20.8581 mL	104.2905 mL
5 mM	0.4172 mL	2.0858 mL	4.1716 mL	20.8581 mL
10 mM	0.2086 mL	1.0429 mL	2.0858 mL	10.4291 mL
20 mM	0.1043 mL	0.5215 mL	1.0429 mL	5.2145 mL
50 mM	0.0417 mL	0.2086 mL	0.4172 mL	2.0858 mL
100 mM	0.0209 mL	0.1043 mL	0.2086 mL	1.0429 mL