YUM70
目录号: PL03737 纯度: ≥98%
CAS No. :423145-35-1
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中文名称
YUM70
英文名称
YUM70
英文别名
MLS000548411;SMR000172091;N-[Benzo[1,3]dioxol-5-yl-(5-chloro-8-hydroxy-quinolin-7-yl)-methyl]-butyramide;BAS 02169251;Oprea1_596028;Oprea1_626646;BDBM77529;cid_3138755;HMS2575N03;DNDI1417995;N-[1,3-benzodioxol-5-yl-(5-chloro-8-hydroxyquinolin-7-yl)methyl]butanamide;N-[1,3-benzodioxol-5-yl-(5-chloro-8-hydroxy-7-quinolinyl)methyl]butanamide;N-[1,3-benzodioxol-5-yl-(5-chloro-8-hydroxy-7-quinolyl)methyl]butyramide;N-(Benzo[d][1,3]dioxol-5-y;YUM70
Cas No.
423145-35-1
分子式
C21H19ClN2O4
分子量
398.84
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
YUM70 是一种有效和选择性的葡萄糖调节蛋白 78 (GRP78) 抑制剂,抑制全长蛋白的 GRP78 ATPase 活性的 IC50 值为 1.5 μM。YUM70 可诱导内质网 (ER) 应激介导的胰腺癌细胞凋亡。YUM70 在胰腺癌异种移植模型中也具有体内功效。
生物活性
YUM70 is a potent and selective inhibitor of glucose-regulated protein 78 (GRP78), with an IC 50 of 1.5 μM for inhibiting GRP78 ATPase activity of the full-length protein. YUM70 induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer. YUM70 also has in vivo efficacy in a pancreatic cancer xenograft model.
性状
Solid
IC50 & Target[1][2]
IC50: 1.5 μM (glucose-regulated protein 78)
体外研究(In Vitro)
YUM70 shows selective cytotoxicity for MIA PaCa-2, PANC-1, BxPC-3 cells (IC50=2.8, 4.5, and 9.6 μM, respectively) over normal pancreatic tissue-derived HPNE cells (IC50>30 μM).
YUM70 (5 μM; 24 h) induces endoplasmic reticulum (ER) stress-mediated apoptosis of MIA PaCa-2cells. has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis
体内研究(In Vivo)
YUM70 (30 mg/kg; i.p. 5 days a week for 7 weeks) inhibits tumor growth in a MIA PaCa-2 xenograft model.
YUM70 (15 mg/kg; i.v.) exhibits t 1/2 (1.40 h), CL (724.04 mL/h/kg), and V ss (1162.73 mL/kg) in mice.
YUM70 (30 mg/kg; p.o.) exhibits bioavailability (6.71%), t 1/2 (2.74 h), and CL (9230.15 mL/h/kg) in 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
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Samanta S, et, al. The hydroxyquinoline analog YUM70 inhibits GRP78 to induce ER stress-mediated apoptosis in pancreatic cancer. Cancer Res. 2021 Feb 2;canres.1540.2020.
溶解度数据
In Vitro: DMSO : 100 mg/mL (250.73 mM; Need ultrasonic)配制储备液
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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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