GCN2iB ( —— )

产品货号. M26229 CAS No. 2183470-12-2

GCN2iB 是一种 ATP 竞争性的一般控制非阻抑物 2 (GCN2) 抑制剂，IC50 为 2.4 nM。

纯度: >98% (HPLC)

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

规格	价格/人民币	库存	数量
5MG	￥1442	有现货
10MG	￥2333	有现货
25MG	￥4666	有现货
50MG	￥6683	有现货
100MG	￥9153	有现货
200MG	获取报价	有现货
500MG	获取报价	有现货
1G	获取报价	有现货

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生物学信息

产品名称

GCN2iB
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

GCN2iB 是一种 ATP 竞争性的一般控制非阻抑物 2 (GCN2) 抑制剂，IC50 为 2.4 nM。
产品描述

GCN2iB is an ATP-competitive inhibitor of general control nonderepressible 2 (GCN2) with an IC50 of 2.4 nM.(In Vitro):GCN2iB shows an IC50 value of 2.4 nM for GCN2 and potent cellular activity.?In a panel of 468 kinases, only GCN2 shows >99.5% inhibition, and three kinases (MAP2K5, STK10, and ZAK) show >95%inhibition at 1 μM GCN2iB, demonstrating high kinase selectivity.(In Vivo):In the antitumor activity study of the CCRF-CEM xenografts, ASNase or GCN2iB alone does not significantly affect tumor growth.?Notably, a combination of ASNase and GCN2iB elicits potent antitumor activity (P=0.0002) with synergistic effects.?In MV-4-11 and SU.86.86 xenografts, the robust antitumor activity of the combination of GCN2iB and ASNase is observed with a synergistic effect, respectively.?ASNase/GCN2iB-treated tumors do not show significant growth even after drug cessation.
体外实验

GCN2iB shows an IC50 value of 2.4 nM for GCN2 and potent cellular activity. In a panel of 468 kinases, only GCN2 shows >99.5% inhibition, and three kinases (MAP2K5, STK10, and ZAK) show >95%inhibition at 1 μM GCN2iB, demonstrating high kinase selectivity.
体内实验

In the antitumor activity study of the CCRF-CEM xenografts, ASNase or GCN2iB alone does not significantly affect tumor growth. Notably, a combination of ASNase and GCN2iB elicit potent antitumor activity (P=0.0002) with synergistic effects. In MV-4-11 and SU.86.86 xenografts, robust antitumor activity of the combination of GCN2iB and ASNase is observed with synergistic effect, respectively. ASNase/GCN2iB-treated tumors do not show significant growth even after drug cessation. The combination of ASNase and GCN2iB yield survival advantage compared with the vehicle treated control with synergistic effect.
同义词

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通路

Others
靶点

Other Targets
受体

Antibacterial
研究领域

——
适应症

——

化学信息

CAS Number

2183470-12-2
分子量

451.83
分子式

C18H12ClF2N5O3S
纯度

>98% (HPLC)
溶解度

In Vitro:?DMSO : 50 mg/mL (110.66 mM)
SMILES

COc1ncc(Cl)cc1S(=O)(=O)Nc1ccc(F)c(C#Cc2cnc(N)nc2)c1F
化学全称

——

运输与储存

储存条件

(-20℃)
运输条件

With Ice Pack
稳定性

≥ 2 years

参考文献

1.Losch K. [Pharmacokinetic studies of sulfamerazine-Na, sulfaperine-Na and sulfadimidine-Na in the hen]. Arch Exp Veterinarmed. 1980;34(4):587-94. German.

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摩尔计算器

分子量计算器

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