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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-ERK-ASN007
ASN007

Chemical Structure : ASN007

CAS No.: 2055597-12-9

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ASN007 (ASN-007, ASN 007)

货号: PC-72428Not For Human Use, Lab Use Only.

ASN007 (ASN-007) is a potent, selective, orally bioavailable ERK1/2 inhibitor with IC50 of 2 nM against both.

规格 价格 库存 数量
5 mg ￥1280 In stock
10 mg ￥1980 In stock
25 mg ￥3480 In stock
50 mg ￥5580 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

ASN007 (ASN-007) is a potent, selective, orally bioavailable ERK1/2 inhibitor with IC50 of 2 nM against both.
ASN007 demonstrated a selective inhibition of ERK1/2 kinases at 1 uM in a panel of 335 serine/threonine, tyrosine, and protein lipid kinases.
ASN007 shows strong antiproliferative activity in cancer cells harboring mutations in BRAF and RAS (KRAS, NRAS, and HRAS) with median IC50 of 37 nM (range, 13-100 nM), without effect againstcell lines without the mutations (IC50>10,000 nM).
ASN007 demonstrates activity in a BRAFV600E mutant melanoma tumor model that is resistant to BRAF and MEK inhibitors.
The PI3K inhibitor copanlisib enhances the antiproliferative activity of ASN007 both in vitro and in vivo due to dual inhibition of RAS/MAPK and PI3K survival pathways, decreases the phosphorylation of ERK1/2 target proteins RSK and MSK.

物理化学性质&存储条件

分子量 473.937
分子式 C22H25ClFN7O2
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

N-(2-amino-1-(3-chloro-5-fluorophenyl)ethyl)-1-(5-methyl-2-((tetrahydro-2H-pyran-4-yl)amino)pyrimidin-4-yl)-1H-imidazole-4-carboxamide

参考文献

1. Ana Portelinha, et al. Cell Rep Med. 2021 Jul 21;2(7):100350.

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