Product Details
| Product Name:
Temuterkib |
CAS No.:
1951483-29-6 |
| Purity:
99.76% |
Supply Ability:
10g |
| Release date:
2024/11/01 |
Product Introduction
Bioactivity
| 名稱 | Temuterkib |
| 描述 | Temuterkib (LY3214996) is a potent and selective, orally available inhibitor of the extracellular signal-regulated kinase (ERK) 1 and 2, with potential antineoplastic activity. |
| 體外活性 | 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]. |
| 體內(nèi)活性 | In tumor xenograft models, LY3214996 effectively inhibits the PD biomarker phospho-p90RSK1 and its PD effects, correlating with compound exposure and antitumor activity. It demonstrates comparable or superior efficacy to existing ERK inhibitors in BRAF or RAS mutant cell lines and xenografts. Oral administration of LY3214996 notably suppresses tumor growth across various cancer xenografts, including BRAF or NRAS mutant melanoma, and BRAF or KRAS mutant colorectal, lung, and pancreatic cancers, showing good tolerance. It offers a promising therapeutic strategy for cancers linked to MAPK pathway alterations. Remarkably, LY3214996 also counters Vemurafenib-resistant A375 melanoma xenografts, highlighting its potential in treating melanoma patients unresponsive to BRAF therapy. Furthermore, LY3214996 can be used alongside investigational and approved treatments, especially in KRAS mutant cases. Its combination with the CDK4/6 inhibitor abemaciclib exhibits significant tumor growth inhibition or regression in diverse cancer models, including KRAS mutant colorectal and non-small cell lung cancers, showcasing its broad therapeutic potential[1]. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 4.54 mg/mL (10 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
|
| 關(guān)鍵字 | inhibit | Extracellular signal regulated kinases | Temuterkib | LY-3214996 | LY 3214996 | Inhibitor | ERK |
| 相關(guān)產(chǎn)品 | TBHQ | Notoginsenoside R1 | Lidocaine | Ro-3306 | Astragaloside IV | Olomoucine | Lidocaine hydrochloride | Selumetinib | Tauroursodeoxycholate sodium | Honokiol | Tauroursodeoxycholate | ROCK-IN-5 |
| 相關(guān)庫 | 高選擇性抑制劑庫 | 疼痛相關(guān)化合物庫 | 經(jīng)典已知活性庫 | 激酶抑制劑庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | 抗衰老化合物庫 | 已知活性化合物庫 | 抗癌藥物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
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|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States