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GSK2008607

Name: GSK2008607
Brand: TargetMol
SKU: T27454
Price: 2350 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.99%

货号 T27454Cas号 1244644-50-5

GSK2008607是一种有效的 B-RafV600E 抑制剂，具有抗癌活性，可用来研究乳腺癌、结直肠癌、黑色素瘤、甲状腺癌、卵巢癌。

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GSK2008607

一键复制产品信息

很棒

纯度: 99.99%

货号 T27454Cas号 1244644-50-5

GSK2008607是一种有效的 B-RafV600E 抑制剂，具有抗癌活性，可用来研究乳腺癌、结直肠癌、黑色素瘤、甲状腺癌、卵巢癌。

规格	价格	库存
1 mg	¥ 2,350	现货
5 mg	¥ 5,630	现货
10 mg	¥ 7,790	现货
25 mg	¥ 11,200	现货
50 mg	¥ 13,800	现货
100 mg	¥ 17,500	现货
500 mg	¥ 34,800	现货

库存状态实时更新，以官网显示为准，现货产品可直接加购物车下单

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纯度: 99.99%

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COA LCMS HNMR 产品操作手册

产品介绍

GSK2008607 AI Summary

GSK2008607 demonstrates significant bioactivity across multiple assays and species. It exhibits intrinsic clearance in rat liver microsomes at a rate of 10.0 mL.min-1.g-1. The compound shows potent antiproliferative activity against human SK-MEL-28 cells expressing the B-Raf V600E mutant, with an EC50 of 8.0 nM after 3 days. Additionally, it effectively inhibits ERK phosphorylation in these cells with an EC50 of 11.0 nM after 1 hour and directly inhibits the B-Raf V600E mutant with an IC50 of 0.5 nM. In pharmacokinetic studies, GSK2008607 has high oral bioavailability in rats (85.0%), but much lower bioavailability in monkeys (5.0%) and dogs (10.0%). The dose-normalized AUC values are significantly higher in rats (1748.0 ng.hr/ml/mg/kg) compared to monkeys (23.0 ng.hr/ml/mg/kg) and dogs (42.0 ng.hr/ml/mg/kg). Blood clearance is highest in monkeys (39.0 mL.min-1.kg-1) followed by dogs (38.0 mL.min-1.kg-1) and rats (9.0 mL.min-1.kg-1). The compound shows marginal to moderate bioactivity in reducing the motility of O. lienalis microfilariae, with a 93.4% reduction, and has been tested for cytotoxicity against Rhesus Monkey LLCMK2 cells. In terms of inhibition of NEK proteins, GSK2008607 exhibits very high inhibition of NEK3 (99.0%) and NEK10 (100.0%), moderate inhibition of NEK4 (49.0%) and NEK5 (24.0%), and lower inhibition of NEK7 (7.1%), NEK9 (6.4%), and NEK11 (1.4%). Minimal inhibition is observed on NEK2 and NEK6 (0.9% each). These results indicate GSK2008607's potential as a targeted inhibitor, particularly against NEK3 and NEK10, as well as its potent anticancer activity through B-Raf V600E mutant inhibition..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	GSK2008607 is a potent B-RafV600E inhibitor with anticancer activity and can be used to study breast, colorectal, melanoma, thyroid, and ovarian cancers.
靶点活性	B-Raf:0.008 µM(EC50), B-Raf:< 0.1 µM

化学信息

分子量	667.72
分子式	C₃₁H₂₈F₃N₇O₃S₂
CAS No.	1244644-50-5
Smiles	C(C)(C)C=1SC(=C(N1)C2=C(F)C(NS(=O)(=O)C3=C(F)C=CC=C3F)=CC=C2)C4=NC(NC=5C=CC(=NC5)N6CCOCC6)=NC=C4
密度	no data available

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 50 mg/mL (74.88 mM), Sonication is recommended.

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.4976 mL	7.4882 mL	14.9763 mL	74.8817 mL
5 mM	0.2995 mL	1.4976 mL	2.9953 mL	14.9763 mL
10 mM	0.1498 mL	0.7488 mL	1.4976 mL	7.4882 mL
20 mM	0.0749 mL	0.3744 mL	0.7488 mL	3.7441 mL
50 mM	0.0300 mL	0.1498 mL	0.2995 mL	1.4976 mL

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：

比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10只，您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH₂O，那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 100 μL DMSO （母液浓度为 20 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们联系。