货号	规格	价格	上海	北京	珠海	重庆	武汉
S88367-5mg买3赠1	99.50%	￥420.00 S88367-5mg ￥420.00 现货（买3赠1）	8 8	-	-	-	-
S88367-10mg买3赠1	99.50%	￥660.00 S88367-10mg ￥660.00 现货（买3赠1）	6 6	-	-	-	-
S88367-25mg促销	99.50%	￥1340.00 ￥1070.00 S88367-25mg ￥1070.00 现货	6 6	-	-	-	-
S88367-50mg促销	99.50%	￥2140.00 ￥1710.00 S88367-50mg ￥1710.00 现货	4 4	-	-	-	-
S88367-100mg促销	≥98%	￥3120.00 ￥2490.00 S88367-100mg ￥2490.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

Longdaysin is an inhibitor of CK1α and CK1δ (IC50s: 5.6/8.8 μM). It also can inhibit ERK2 (IC50: 52 μM)

靶点：

ERK; Casein Kinase; CDK;ERK; CaseinKinase; CDK

体外研究：

Longdaysin inhibited CKIδ, CKIα, ERK2, and CDK7 activities (IC50 = 8.8, 5.6, 52, and 29 µM, respectively), while it had much less effect on p38α. The period of CKIδ deficient cells was 1.1 h longer than that of wild type cells. Longdaysin lengthened the period in a dose-dependent manner in CKIδ deficient cells as well as in wild type cells [1]. In breast cancer Hs578T and MDA-MB-231 cells, micromolar concentrations of longdaysin attenuated the phosphorylation of LRP6 and DVL2 and reduced the expression of active β-catenin and total β-catenin, leading to the downregulation of Wnt target genes Axin2, DKK1, LEF1, and Survivin

体内研究：

In MDA-MB-231 breast cancer xenografts, treatment with longdaysin suppressed tumor growth in association with inhibition of Wnt/β-catenin signaling

细胞实验：

2×10^5 cells were suspended in 100 μL serum-free medium containing the indicated concentrations of longdaysin, and then seeded in 24-transwell chambers with 8 μm pore membrane. The lower chamber contained medium with 20% FBS. After incubation at 37°C for 6 hours, the unmigrated cells on the upper side of membrane were removed by a cotton swab, and the migrated cells were stained with crystal violet and stained cells were photomicrographed. For invasion assays, the transwell chambers with 8 μm pore membranes were coated with Matrigel

动物实验：

MDA-MB-231 cells were injected s.c. into the right flank of nude mice (1×10^7 cells per mouse), and tumor growth was closely observed and measured every 3 days. When the tumors reached approximately 50 mm3, the mice were randomly divided into two groups (eight mice per group) and i.p. injected with the vehicle (0.8% DMSO/12% Cremophor/8% ethanol in normal saline) or 5 mg/kg longdaysin in vehicle every 3 days. This longdaysin dosage was selected based on results from preliminary experiments, and was well tolerated in the mouse model. Subsequently, tumor volumes were measured with a caliper and calculated as follows: 0.523×(length)×(width)2. After treatment for 3 weeks, the mice were sacrificed and the tumor tissues were collected and weighed before being fixed in buffered formalin

参考文献：

1. Xiong Y, et al. Longdaysin inhibits Wnt/β-catenin signaling and exhibits antitumor activity against breast cancer. Onco Targets Ther. 2019 Feb 5;12:993-1005. 2. Hirota T, et al. High-throughput chemical screen identifies a novel potent modulator of cellular circadian rhythms and reveals CKIα as a clock regulatory kinase. PLoS Biol. 2010 Dec 14;8(12):e1000559.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.982 ml	14.911 ml	29.822 ml
5 mM	0.596 ml	2.982 ml	5.964 ml
10 mM	0.298 ml	1.491 ml	2.982 ml
50 mM	0.06 ml	0.298 ml	0.596 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置

LONGDAYSIN

9H-Purin-6-aMine, 9-(1-Methylethyl)-N-[[3-(trifluoroMethyl)phenyl]Methyl]-

参考文献

质检证书(COA)

如何获取质检证书(COA)?

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)