GSK2606414 纯度: 99.76%
GSK2606414 是可渗透细胞且有口服活性的蛋白激酶 R 样内质网 (ER) 激酶 (PERK) 抑制剂,IC50值为 0.4 nM。
GSK2606414 Chemical Structure
CAS No. : 1337531-36-8
规格 | 价格 | 是否有货 | 数量 |
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Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥1092 | In-stock | |
2 mg | ¥700 | In-stock | |
5 mg | ¥1100 | In-stock | |
10 mg | ¥1500 | In-stock | |
50 mg | ¥5500 | In-stock | |
100 mg | ¥8500 | In-stock | |
200 mg | ¥12000 | In-stock | |
500 mg | 询价 | ||
1 g | 询价 |
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生物活性 |
GSK2606414 is a cell-permeable and orally available protein kinase R-like endoplasmic reticulum (ER) kinase (PERK) inhibitor with an IC50 of 0.4 nM. |
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IC50 & Target[1] |
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体外研究 (In Vitro) |
GSK2606414 inhibits PERK activation in cells[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
GSK2606414 (50 and 150 mg/kg, p.o.) inhibits the growth of a human tumor xenograft in mice[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
451.44 |
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Formula |
C24H20F3N5O |
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CAS 号 |
1337531-36-8 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : ≥ 100 mg/mL (221.51 mM) * “≥” means soluble, but saturation unknown. 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Animal Administration [1] |
Exponentially growing BxPC3 tumor cells (10×106 cells/mouse) from cell culture are implanted subcutaneously into the right flank of female nude mice. Sixteen days after implantation, mice with -200 mm3 tumors are randomized into various treatment groups (n=8 mice/group). Animals are orally treated with vehicle (0.5% hydoxypropylmethylcellulose, 0.1% Tween 80 in water, pH 4.8), compound at 50 or 150 mg/kg, b.i.d. for 21 days. Tumor volume is measured twice weekly with calipers and calculated. Results are represented as percent inhibition on completion of dosing, which is 100[1-(average growth of drug-treated population)/(average growth of vehicle-treated control population)]. Statistical analysis is performed using a two-tailed t test. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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参考文献 |
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