货号	规格	价格	上海	北京	珠海	重庆	武汉
S84205-1mg买3赠1	99.80%	￥320.00 S84205-1mg ￥320.00 现货（买3赠1）	5 5	-	-	-	-
S84205-2mg买3赠1	99.80%	￥450.00 S84205-2mg ￥450.00 现货（买3赠1）	5 5	-	-	-	-
S84205-5mg买3赠1	99.80%	￥740.00 S84205-5mg ￥740.00 现货（买3赠1）	3 3	-	-	-	-
S84205-10mg买3赠1	99.80%	￥1300.00 S84205-10mg ￥1300.00 现货（买3赠1）	6 6	-	-	-	-
S84205-25mg买3赠1	99.80%	￥2900.00 S84205-25mg ￥2900.00 现货（买3赠1）	6 6	-	-	-	-
S84205-50mg	99.80%	￥5000.00 S84205-50mg ￥5000.00 现货	4 4	-	-	-	-
S84205-100mg	≥99%	￥8900.00 S84205-100mg ￥8900.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

Temuterkib (LY3214996) is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. Temuterkib potently inhibits cellular p-RSK1 in BRAF and RAS mutant cancer cell lines. Temuterkib shows potent antitumor activities in cancer models with MAPK pathway alterations.

靶点：

ERK1:5 nM (IC50);ERK2:5 nM (IC50);ERK

体外研究：

Temuterkib is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. Temuterkib potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines. In an unbiased tumor cell panel sensitivity profiling for inhibition of cell proliferation, tumor cells with MAPK pathway alterations including BRAF, NRAS or KRAS mutation are generally sensitivity to Temuterkib

体内研究：

In tumor xenograft models, Temuterkib inhibits PD biomarker phospho-p90RSK1 in tumors and the PD effects are correlated with compound exposures and anti-tumor activities. Temuterkib shows either similar or superior anti-tumor activity as compared to other published ERK inhibitors in BRAF or RAS mutant cell lines and xenograft models. Oral administration of single-agent Temuterkib significantly inhibits tumor growth in vivo and is well tolerated in BRAF or NRAS mutant melanoma, BRAF or KRAS mutant colorectal, lung and pancreatic cancer xenografts or PDX models. Therefore, Temuterkib can be tailored for treatment of cancers with MAPK pathway alteration. In addition, Temuterkib has anti-tumor activity in a PLX4032-resistant A375 melanoma xenograft model due to MAPK reactivation, may have potential for treatment of melanoma patients who have failed BRAF therapies. More importantly, Temuterkib can be combined with investigational and approved agents in preclinical models, particularly KRAS mutant models. Combination treatment of Temuterkib and CDK4/6 inhibitor abemaciclib is well tolerated and results in potent tumor growth inhibition or regression in multiple in vivo cancer models, including KRAS mutant colorectal and non-small cell lung cancers

参考文献：

1. Shripad V. Bhagwat, et al. Abstract 4973: Discovery of LY3214996, a selective and novel ERK1/2 inhibitor with potent antitumor activities in cancer models with MAPK pathway alterations. Cancer Research. July 2017.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.205 ml	11.024 ml	22.048 ml
5 mM	0.441 ml	2.205 ml	4.41 ml
10 mM	0.22 ml	1.102 ml	2.205 ml
50 mM	0.044 ml	0.22 ml	0.441 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(1篇)

1. [IF=4.9] Xin Li et al."Paeonol Relieves Chronic Neuropathic Pain by Reducing Communication Between Schwann Cells and Macrophages in the Dorsal Root Ganglia After Injury."INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES.2025 Jan;26(9):3964

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