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CAS No.: 1257423-87-2

BTdCPU Catalog No. CSN24724

Synonyms: heme-regulated inhibitor kinase activator;eIF2-GTP-tRNAi^Met ternary complex Inhibitor

BTdCPU is acts as an inhibitor of the formation of the ternary complex of eukaryotic translation initiation factor 2 (eIF2), GTP and the initiator methionine tRNA (Met-tRNAi), a key regulatory step of translation initiation.

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技术信息

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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9481 mL
- 14.7406 mL
- 29.4811 mL
- 5 mM
- 0.5896 mL
- 2.9481 mL
- 5.8962 mL
- 10 mM
- 0.2948 mL
- 1.4741 mL
- 2.9481 mL

技术信息

CAS号

1257423-87-2

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H8Cl2N4OS

运输

蓝冰

分子量

339.20

别名

heme-regulated inhibitor kinase activator;eIF2-GTP-tRNAi^Met ternary complex Inhibitor

溶解度

DMSO	21.0 mg/mL (61.9 mM)
Water	insoluble

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