Glutaminase-IN-1 (Synonyms: CB839 derivative)
目录号: PL02202 纯度: ≥98%
CAS No. :2247127-79-1
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中文名称
Glutaminase-IN-1
英文名称
Glutaminase-IN-1
英文别名
Glutaminase-IN-1;CB839 derivative;BDBM50517275;N-[6-[4-[5-[(2-pyridin-2-ylacetyl)amino]-1,3,4-selenadiazol-2-yl]butyl]pyridazin-3-yl]-2-[3-(trifluoromethoxy)phenyl]acetamide
Cas No.
2247127-79-1
分子式
C26H24F3N7O3Se
分子量
618.47
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Glutaminase-IN-1 (CB839 derivative) 是CB839 的一个衍生物,是1,3,4-硒二氮基肾型谷氨酰胺酶(KGA) 的变构抑制剂,其IC50 值为1 nM。Glutaminase-IN-1 (CB839 derivative) 具有提高细胞摄取和抗肿瘤的活性。
生物活性
Glutaminase-IN-1 (CB839 derivative), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC 50 of 1 nM. Glutaminase-IN-1 (CB839 derivative) shows improved cellular uptake and antitumor activity.
性状
Solid
IC50 & Target[1][2]
IC50: 1 nM (KGA).
体外研究(In Vitro)
Glutaminase-IN-1 (CPD20), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC50 of 1 nM. Glutaminase-IN-1 shows improved cellular uptake and antitumor activity. The IC50 values of Glutaminase-IN-1 are 17 nM, 6.78 μM, 19 nM and 9 nM in A549, H2, Caki-1 and HCT116 cell lines, respectively. Glutaminase-IN-1 has better KGA inhibitory activity than the corresponding BPTES and CB839. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Glutaminase-IN-1(10 mg/kg, s.c.) reduced the size and weight of the HCT116 tumor, and statistical analysis showed that the 40% reduction in tumor weight by CPD20 is statistically significant. Glutaminase-IN-1 could statistically significantly prolong the survival of H22-bearing mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Chen Z, et al. Novel 1,3,4-Selenadiazole Containing Kidney-Type Glutaminase Inhibitors Showed Improved Cellular Uptake and Antitumor Activity. J Med Chem. 2018 Dec 13.
溶解度数据
In Vitro: DMSO : 125 mg/mL (202.11 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)配制储备液
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2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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