YUM70

目录号: PL03737 纯度: ≥98%
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。
CAS No. :423145-35-1
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PL03737-5mg 5mg ¥2571.00 请登录
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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
详情描述
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。
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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