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BTdCPU

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Chemical Structure| 1257423-87-2 同义名 : -
CAS号 : 1257423-87-2
货号 : A1191670
分子式 : C13H8Cl2N4OS
纯度 : 99%+
分子量 : 339.2
MDL号 : MFCD32004476
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 120 mg/mL(353.77 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:
生物活性
描述 BTdCPU is a potent heme-regulated eIF2α kinase (HRI) activator and promotes eIF2α phosphorylation. BTdCPU induces apoptosis in resistant cell. Combination therapy with rapamycin, an mTOR inhibitor, and BTdCPU, an activator of HRI (heme-regulated eIF2α kinase), demonstrated additive effects on apoptosis in dex-resistant cells. Thus, specific activation of the eIF2α kinase HRI is a novel therapeutic target in MM that can augment current treatment strategies[1]. Treatment with 100, 200 or 350 mg per kg body weight per day of BTdCPU had no discernable adverse effect on weight gain, and mice did not show any outward signs of toxicity, even at the highest dose. Administration of 175 mg per kg per day of BTdCPU caused total tumor stasis starting 1 week after the first injection. Treatment with compound BTdCPU significantly elevated phosphorylation of eIF2α[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.95mL

0.59mL

0.29mL

14.74mL

2.95mL

1.47mL

29.48mL

5.90mL

2.95mL

参考文献

[1]Burwick N, Zhang MY, de la Puente P, et al. The eIF2-alpha kinase HRI is a novel therapeutic target in multiple myeloma. Leuk Res. 2017;55:23-32

[2]Chen T, Ozel D, Qiao Y, et al. Chemical genetics identify eIF2α kinase heme-regulated inhibitor as an anticancer target. Nat Chem Biol. 2011;7(9):610-616. Published 2011 Jul 17