货号	规格	价格	上海	北京	珠海	重庆	武汉
S81043-10mg买3赠1	99.70%	￥282.00 S81043-10mg ￥282.00 现货（买3赠1）	2 2	-	-	-	-
S81043-50mg买3赠1	99.70%	￥650.00 S81043-50mg ￥650.00 现货（买3赠1）	3 3	-	-	-	-
S81043-250mg买3赠1	99.70%	￥1690.00 S81043-250mg ￥1690.00 现货（买3赠1）	4 4	-	-	-	-

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产品描述：

Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis

靶点：

MEK1:2 nM (IC50);MEK2:2 nM (IC50);Apoptosis; MEK; Autophagy

体内研究：

Adjuvant-induced arthritis (AIA) and type II collageninduced arthritis (CIA) development are suppressed almost completely by 0.1 mg/kg of Trametinib (GSK1120212; JTP-74057) or 10 mg/kg of HWA486. Trametinib (0.3 mg/kg, 1 mg/kg, p.o.) is effective in inhibiting the HT-29 xenograft growth in a nude mouse xenograft model.

参考文献：

1. Yamaguchi T, et al. Suppressive effect of an orally active MEK1/2 inhibitor in two different animal models for rheumatoid arthritis: a comparison with HWA486. Inflamm Res, 2012, 61(5), 445-454. 2. Yamaguchi T, et al. Antitumor activities of JTP-74057 (GSK1120212), a novel MEK1/2 inhibitor, on colorectal cancer cell lines in vitro and in vivo. Int J Oncol, 2011, 39(1), 23-31. 3. Abe H, et al. Discovery of a Highly Potent and Selective MEK Inhibitor: GSK1120212 (JTP-74057 DMSO Solvate). ACS Med Chem Lett. 2011 Feb 28;2(4):320-4. 4. Liu H, et al. Identifying and Targeting Sporadic Oncogenic Genetic Aberrations in Mouse Models of Triple Negative Breast Cancer. Cancer Discov. 2018 Mar;8(3):354-369. 5. Lai J, et al. Elimination of melanoma by sortase A-generated TCR-like antibody-drug conjugates (TL-ADCs) targeting intracellular melanoma antigen MART-1. Biomaterials. 2018 Sep;178:158-169.

溶解性：

DMSO : 25 mg/mL (40.62 mM; ultrasonic and warming and heat to 60°C)

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.625 ml	8.125 ml	16.25 ml
5 mM	0.325 ml	1.625 ml	3.25 ml
10 mM	0.162 ml	0.812 ml	1.625 ml
50 mM	0.032 ml	0.162 ml	0.325 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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Trametinib (GSK1120212)