Enpp-1-IN-12

目录号: PL09663 纯度: ≥99%
Enpp-1-IN-12 (化合物 43) 是一种有效和具有口服活性的外核苷酸焦磷酸酶/磷酸二酯酶 1 (ENPP1) 抑制剂,Ki 值 41 nM。Enpp-1-IN-12 具有抗肿瘤活性。
CAS No. :2631703-41-6
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中文名称
Enpp-1-IN-12
英文名称
Enpp-1-IN-12
英文别名
Butanamide, 2-[(2-amino-9H-purin-6-yl)thio]-N-(4-hydroxy-3-methoxyphenyl)-
Cas No.
2631703-41-6
分子式
C16H18N6O3S
分子量
374.42
包装储存
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
详情描述
Enpp-1-IN-12 (化合物 43) 是一种有效和具有口服活性的外核苷酸焦磷酸酶/磷酸二酯酶 1 (ENPP1) 抑制剂,Ki 值 41 nM。Enpp-1-IN-12 具有抗肿瘤活性。
产品详情
Enpp-1-IN-12 (化合物 43) 是一种有效和具有口服活性的外核苷酸焦磷酸酶/磷酸二酯酶 1 (ENPP1) 抑制剂,Ki 值 41 nM。Enpp-1-IN-12 具有抗肿瘤活性。
生物活性
Enpp-1-IN-12 (compound 43) is a potent and orally active ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) inhibitor, with a Ki of 41 nM. Enpp-1-IN-12 exhibits anti-tumor activity.
性状
Solid
IC50 & Target[1][2]
Ki: 41 nM (ENPP1)
体外研究(In Vitro)
Enpp-1-IN-12 (5 μM) exhibits half-life and intrinsic clearance of >120 min and <11.55 μL/min/million cells and 61.88 min and 22.4 μL/min/million cells in human and mouse hepatocytes, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Enpp-1-IN-12 (100 mg/kg; p.o.) inhibits tumor growth in LLC1 syngeneic murine tumor model for lung cancer.
Enpp-1-IN-12 (10 mg/kg; p.o.) exhibits moderate oral bioavailability (F=45.1%), half-life (t 1/2 =1.04 h), and C max (303.10 ng/mL) in healthy female BALB/c mice.
Enpp-1-IN-12 (1 mg/kg; i.v.) exhibits half-life (t 1/2 =0.76 h), C max (308.64 ng/mL), and CL of 73.22 mL/min/kg in healthy female BALB/c 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
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献
[1]. Gangar M, et, al. Design, synthesis and biological evaluation studies of novel small molecule ENPP1 inhibitors for cancer immunotherapy. Bioorg Chem. 2022 Feb;119:105549.
溶解度数据
In Vitro: DMSO : 50 mg/mL (133.54 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)
[1]. Gangar M, et, al. Design, synthesis and biological evaluation studies of novel small molecule ENPP1 inhibitors for cancer immunotherapy. Bioorg Chem. 2022 Feb;119:105549.

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

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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