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CHS-828 (Synonyms: GMX1778) 纯度: 99.35%
CHS-828 (GMX1778) 是一种竞争性的烟酰胺磷酸化转移酶抑制剂 (NAMPT),IC50 值 <25 nm。chs-828 (gmx1778) 通过降低细胞中的 nad+ 水平发挥细胞毒性作用,具有较强的抗癌活性。
CHS-828 Chemical Structure
CAS No. : 200484-11-3
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 | ¥715 | In-stock | |
5 mg | ¥650 | In-stock | |
10 mg | ¥870 | In-stock | |
50 mg | ¥3220 | In-stock | |
100 mg | 询价 | ||
200 mg | 询价 |
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CHS-828 相关产品
•相关化合物库:
- Clinical Compound Library Plus
- Bioactive Compound Library Plus
- Apoptosis Compound Library
- Metabolism/Protease Compound Library
- Anti-Cancer Compound Library
- Clinical Compound Library
生物活性 |
CHS-828 (GMX1778) is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), with an IC50 less than 25 nM. CHS-828 (GMX1778) exerts a cytotoxic effect by decreasing the cellular level of NAD+ and exhibits a potent anticancer activity[1]. |
IC50 & Target |
IC50: < 25 nM (NAMPT)[1]. |
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体外研究 (In Vitro) |
The phosphoribosyltransferase activity of recombinant NAMPT was sensitive to inhibition by CHS-828 (GMX1778) (IC50 < 25 nM) whereas the adenyltransferase activity of recombinant NMNAT1 was not. The Kd of recombinant NAMPT for GMX1778 labeled with a fluorescent tag (CHS-828 (GMX1778)-Alexa Fluor) was 120 nM. Overexpression of wild-type NAMPT was able to maintain a certain level of NAD+ under conditions of challenge with 3 nM GMX1778, but this effect was lost when cells were exposed to 300 nM CHS-828 (GMX1778)[1]. CHS-828 (GMX1778) increases intracellular ROS in cancer cells by elevating the superoxide level while decreasing the intracellular NAD(+) level. Notably, CHS-828 (GMX1778) treatment does not induce ROS in normal cells. CHS-828 (GMX1778)-induced ROS can be diminished by adding nicotinic acid (NA) in a NA phosphoribosyltransferase 1 (NAPRT1)-dependent manner[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
A 4-h iv infusion of NA (120 mg/kg of body weight) did not adversely affect the antitumor activity of a 24-h iv infusion of CHS-828 (GMX1778) at a dose of 150 mg/kg or 650 mg/kg in the NAPRT1-deficient xenograft experiments. CHS-828 (GMX1778) at 650 mg/kg is above the maximum tolerated dose. The administration of NA as a 4-h iv infusion immediately following treatment with 750 mg/kg CHS-828 (GMX1778) reduced the mortality associated with toxic doses of GMX1777[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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分子量 |
371.86 |
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Formula |
C19H22ClN5O |
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CAS 号 |
200484-11-3 |
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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 : ≥ 39 mg/mL (104.88 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
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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参考文献 |
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