货号	规格	价格	上海	北京	珠海	重庆	武汉
S88587-1mg买3赠1	99.50%	￥280.00 S88587-1mg ￥280.00 现货（买3赠1）	4 4	-	-	-	-
S88587-5mg买3赠1	99.50%	￥440.00 S88587-5mg ￥440.00 现货（买3赠1）	3 3	-	-	-	-
S88587-10mg买3赠1	99.50%	￥720.00 S88587-10mg ￥720.00 现货（买3赠1）	4 4	-	-	-	-
S88587-25mg促销	99.50%	￥1120.00 ￥896.00 S88587-25mg ￥896.00 现货	6 6	-	-	-	-
S88587-50mg促销	≥98%	￥1920.00 ￥1530.00 S88587-50mg ￥1530.00 2-3天	0 货期：2-3天	-	-	-	-
S88587-100mg促销	≥98%	￥3200.00 ￥2560.00 S88587-100mg ￥2560.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

BI-1347 is an orally active, selective and potent CDK8 inhibitor (IC50=1.1 nM). BI-1347 shows anti-tumoral activity

靶点：

CDK8:1.1 nM (IC50);CDK

体外研究：

BI-1347 (150 nM; 44 h) enhances granzyme B (GZMB+) production in mouse splenic NK cells. BI-1347 (0.1 nM-10 μM; 24 h) treatment increases perforin secretion from NK92MI cells. Western Blot Analysis Cell Line: Mouse splenic NK cells Concentration: 150 nM Incubation Time: 44 hours Result: Increased the proportion of granzyme B-positive NK cells by approximately 4-fold. Western Blot Analysis Cell Line: Human NK92MI cells Concentration: 0.1 nM-10 μM Incubation Time: 24 hours Result: Increased perforin levels with an EC50 value of 7.2 nM.

体内研究：

BI-1347 (oral gavage; 10 mg/kg; once daily; 30 d) modulates STAT1S727 phosphorylation and shows anti-tumor activity in vivo. BI-1347 (oral gavage; 10 mg/kg) intermittent schedule and BI-8382 continuous treatment combination treatment increases efficacy compared to each monotherapy in the mammary carcinoma EMT6 model. Animal Model: B16-F10-luc2 syngeneic melanoma model Dosage: 10 mg/kg Administration: Oral gavage; 10 mg/kg; once daily; 30 d Result: Reduced phosphorylation of STAT1S727 for at least 6 h by 60%.Showed minimal effect on body weight at 10 mg/kg.Showed lower tumor burden both on day 23 and 29, compared to the control group.

参考文献：

1. Harald Engelhardt, et al. New phenylpyrazolylacetamide compounds and derivatives as cdk8/cdk19 inhibitors. 2. Hofmann MH, et al. Selective and Potent CDK8/19 Inhibitors Enhance NK-Cell Activity and Promote Tumor Surveillance. Mol Cancer Ther. 2020 Apr;19(4):1018-1030.

溶解性：

Soluble in DMSO

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.806 ml	14.028 ml	28.057 ml
5 mM	0.561 ml	2.806 ml	5.611 ml
10 mM	0.281 ml	1.403 ml	2.806 ml
50 mM	0.056 ml	0.281 ml	0.561 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

BI-1347

None

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)