ENPP1 Inhibitor C
目录号 : GC46138
ENPP1 Inhibitor C是一种选择性外核苷酸焦磷酸酶/磷酸二酯酶1（ENPP1）抑制剂，对ENPP1的IC50值为10µM。
Cas No.:2378640-92-5
Sample solution is provided at 25 µL, 10mM.
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ENPP1 Inhibitor C is a selective inhibitor of Ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) with an IC50 value of 10µM [1]. ENPP1 Inhibitor C exhibited an IC50 of 2.3µM with cGAMP and 70µM with ATP[1]. ENPP1 Inhibitor C has been used to regulate the cGAS/STING pathway and to synthesize novel fluorescent probes[2].
In vitro, ENPP1 Inhibitor C pretreatment at 300nM for 2h effectively activated STING signaling and stimulated type I IFN responses in THP-1 cells[3].
In vivo, ENPP1 Inhibitor C treatment via subcutaneous injection at a dose of 100mg/kg/day for 21 days significantly inhibited 4T1 tumor growth, resulting in a significant reduction in the number of pulmonary metastatic nodules and intraperitoneal nodules in the murine tumor model[3].
References:
[1] Kumar M, Lowery R G. Development of a high-throughput assay to identify inhibitors of ENPP1[J]. SLAS DISCOVERY: Advancing the Science of Drug Discovery, 2021, 26(5): 740-746.
[2] Kawaguchi M, Han X, Hisada T, et al. Development of an ENPP1 fluorescence probe for inhibitor screening, cellular imaging, and prognostic assessment of malignant breast cancer[J]. Journal of medicinal chemistry, 2019, 62(20): 9254-9269.
[3] Sun Y, Chen M, Han Y, et al. Discovery of Pyrido [2, 3-d] pyrimidin-7-one derivatives as highly potent and efficacious ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) inhibitors for cancer treatment[J]. Journal of Medicinal Chemistry, 2024, 67(5): 3986-4006.
ENPP1 Inhibitor C是一种选择性外核苷酸焦磷酸酶/磷酸二酯酶1（ENPP1）抑制剂，对ENPP1的IC50值为10µM[1]。ENPP1 Inhibitor C对cGAMP和ATP的IC50值分别为2.3µM和70µM[1]。ENPP1 Inhibitor C已被用于调控cGAS/STING通路及新型荧光探针的合成研究[2]。
在体外，300nM浓度的ENPP1 Inhibitor C预处理2小时可有效激活THP-1细胞中的STING信号通路并刺激I型干扰素反应[3]。
在体内，皮下注射ENPP1 Inhibitor C（100mg/kg/day）连续21天能显著抑制小鼠肿瘤模型中的4T1肿瘤生长，并明显减少肺转移结节和腹腔结节数量[3]。
| Animal experiment [1]: | |
Animal models | BALB/c mice |
Preparation Method | A total of 5 × 105 4T1 cells were inoculated into the mammary fat pad of five-week-old female BALB/c mice. When tumor volume reached approximately 60mm3, animals were randomly divided into three groups (six mice per group) and received daily subcutaneous injections of vehicle (PBS) or ENPP1 Inhibitor C at a dose of 100mg/kg/day for 21 days. Body weight and tumor volume were measured and recorded twice a week. Tumor volume was calculated using the following formula: Volume (mm3) = 0.5×length(mm)×width2 (mm2). Relative tumor volume (RTV) was calculated as the ratio of the tumor volume at a given time point to the tumor volume at initial treatment. At the end of the experiment, mice were sacrificed and tumor tissues, lungs, and intestines were collected. The number of metastatic lung and intestinal nodules in each animal was counted visually. It should be noted that one mouse in the solvent group died before the end point of the experiment (24 hours). To ensure sample accuracy, lungs and intestines from dead mice were not collected. |
Dosage form | 100mg/kg/day for 21 days; s.c. |
Applications | ENPP1 Inhibitor C treatment significantly suppressed tumor growth and reduced the number of pulmonary metastatic nodules and intraperitoneal nodules in mice. |
References: | |
| Cas No. | 2378640-92-5 | SDF | |
| Canonical SMILES | NC1=CC=CC(CC2=C(N(C)C)N3C(N=C2C)=NC=N3)=C1 | ||
| 分子式 | C15H18N6 | 分子量 | 282.3 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5423 mL | 17.7117 mL | 35.4233 mL |
| 5 mM | 0.7085 mL | 3.5423 mL | 7.0847 mL |
| 10 mM | 0.3542 mL | 1.7712 mL | 3.5423 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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1. 首先保证母液是澄清的；
2.
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- Purity: >99.00%
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