MKC8866|1338934-59-0|(Orin1001)-陌孚医药/Medlife

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MKC8866 (Synonyms: Orin1001)

目录号: PL01479 纯度: ≥99%

CAS No. :1338934-59-0

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中文名称	MKC8866
英文名称	MKC8866
英文别名	MKC8866;1NZ0YBP9HB;7-hydroxy-6-methoxy-4-methyl-3-(2-morpholino-2-oxoethyl)-2-oxo-2H-chromene-8-carbaldehyde;IRE1 RNase inhibitor 8866;BDBM160445;s8875;US9040714, 167;7-hydroxy-6-methoxy-4-methyl-3-(2-morpholin-4-yl-2-oxoethyl)-2-oxochromene-8-carbaldehyde;2H-1-Benzopyran-8-carboxaldehyde, 7-hydroxy-6-methoxy-4-methyl-3-(2-(4-morpholinyl)-2-oxoethyl)-2-oxo-
Cas No.	1338934-59-0
分子式	C₁₈H₁₉NO₇
分子量	361.35
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	MKC8866 是一种水杨醛类似物，有效的选择性 IRE1 RNase 抑制剂，在体外的 IC₅₀ 为 0.29 μM。 MKC8866 强烈抑制 Dithiothreitol 诱导的 XBP1s 表达，EC₅₀ 为 0.52 μM。MKC8866 抑制无应激 RPMI 8226 细胞，IC₅₀ 为 0.14 μM。 MKC8866 抑制乳腺癌细胞中的 IRE1 RNase 导致促肿瘤发生因子减少，同时也能抑制前列腺癌 (PCa) 肿瘤的生长。
生物活性	MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC 50 of 0.29?μM in human vitro. MKC8866 strongly inhibits Dithiothreitol-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC 50 of 0.52?μM and unstresses RPMI 8226 cells with an IC 50 of 0.14?μM. MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibits prostate cancer (PCa) tumor growth.
性状	Solid
IC50 & Target[1][2]	IC50: 0.29?μM (IRE1 RNase)
体外研究(In Vitro)	MKC8866 (20?μM; 6 days) decreases proliferation of all breast cancer cell lines. MKC8866 (20 μM; 48 hours) reduces the number of cells entering S phase. MKC8866 (0.2-10 μM; 3 days) suppresses the viability of all four cell lines in a dose-dependent manner under normal conditions, with the most robust effect in LNCaP cells. MKC8866 (20 μM; 72?hours) is sufficient to completely block NSC 125973-induced expression of XBP1s . has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	MKC8866 (oral ; 300 mg/kg; for 28 days) reduces tumor regrowth post-NSC 125973 withdrawal. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female athymic nude mice with MDA-MB-231 tum
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]. Sheng X, et al. IRE1α-XBP1s pathway promotes prostate cancer by activating c-MYC signaling. Nat Commun. 2019 Jan 24;10(1):323. [2]. Logue SE, et al. Inhibition of IRE1 RNase activity modulates the tumor cell secretome and enhances response to chemotherapy. Nat Commun. 2018 Aug 15;9(1):3267.

溶解度数据	In Vitro: DMSO : 6.67 mg/mL (18.46 mM; ultrasonic and warming and heat to 60°C)配制储备液

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