上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
Temuterkib (Synonyms: LY3214996) 纯度: 99.85%
Temuterkib (LY3214996) 是高效的选择性 ERK1 和 ERK2 抑制剂,IC50 为 5 nM。Temuterkib 作用于 BRAF 和 RAS 突变癌细胞系中,有效抑制 p-RSK1。Temuterkib 在 MAPK 途径改变的癌症模型中具有强大的抗肿瘤活性。
Temuterkib Chemical Structure
CAS No. : 1951483-29-6
规格 | 价格 | 是否有货 | 数量 |
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10 mM * 1 mL in DMSO | ¥2195 | In-stock | |
1 mg | ¥880 | In-stock | |
5 mg | ¥2200 | In-stock | |
10 mg | ¥3400 | In-stock | |
50 mg | ¥13000 | In-stock | |
100 mg | ¥21000 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
* Please select Quantity before adding items.
Temuterkib 相关产品
•相关化合物库:
- Drug Repurposing Compound Library Plus
- Clinical Compound Library Plus
- Bioactive Compound Library Plus
- Immunology/Inflammation Compound Library
- Kinase Inhibitor Library
- MAPK Compound Library
- Stem Cell Signaling Compound Library
- Anti-Cancer Compound Library
- Clinical Compound Library
- Anti-Aging Compound Library
- Drug Repurposing Compound Library
- Reprogramming Compound Library
- Oxygen Sensing Compound Library
- Glutamine Metabolism Compound Library
- Anti-Lung Cancer Compound Library
- Anti-Pancreatic Cancer Compound Library
- Anti-Obesity Compound Library
- Angiogenesis Related Compound Library
- Anti-Liver Cancer Compound Library
- Anti-Colorectal Cancer Compound Library
生物活性 |
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. |
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IC50 & Target[1] |
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体外研究 (In Vitro) |
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[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
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[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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分子量 |
453.56 |
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Formula |
C22H27N7O2S |
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CAS 号 |
1951483-29-6 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : 20 mg/mL (44.10 mM; Need ultrasonic) 配制储备液
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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