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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-ERK-LY3214996
LY3214996

Chemical Structure : LY3214996

CAS No.: 1951483-29-6

LY3214996 (Temuterkib, LY-3214996)

货号: PC-61973Not For Human Use, Lab Use Only.

Temuterkib (LY-3214996) is a novel potent, selective, orally active ERK1/2 inhibitor with IC50 of 5 nM for both enzymes in biochemical assays.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Temuterkib (LY-3214996) is a novel potent, selective, orally active ERK1/2 inhibitor with IC50 of 5 nM for both enzymes in biochemical assays.
Temuterkib (LY-3214996) potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines.
Temuterkib (LY-3214996) demonstrates inhibition of cell proliferation, general sensitivitity against tumor cells with MAPK pathway alterations including BRAF, NRAS or KRAS mutation.
Temuterkib (LY-3214996) 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.

物理化学性质&存储条件

分子量 453.56
分子式 C22H27N7O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4H-Thieno[2,3-c]pyrrol-4-one,5,6-dihydro-6,6-dimethyl-2-[2-[(1-methyl-1H-pyrazol-5-yl)amino]-4-pyrimidinyl]-5-[2-(4-morpholinyl)ethyl]-

参考文献

1. Shripad V. Bhagwat, et al. AACR Abstract 4973.

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