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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-MAP4K-Famlasertib
Famlasertib

Chemical Structure : Famlasertib

CAS No.: 2375591-69-6

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Famlasertib (Prostetin/12k, Prostetin-12k)

货号: PC-23624Not For Human Use, Lab Use Only.

Famlasertib (Prostetin/12k) is a highly potent, blood-brain barrier-penetrant inhibitor of mitogen-activated protein kinase kinase kinase kinase (MAP4K) family with IC50 of 0.3 nM for HGK (MAP4K4) and 23.7 nM for MLK3.

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5 mg ￥880 In stock
10 mg ￥1280 In stock
25 mg ￥2180 In stock
50 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

Famlasertib (Prostetin/12k) is a highly potent, blood-brain barrier-penetrant inhibitor of mitogen-activated protein kinase kinase kinase kinase (MAP4K) family with IC50 of 0.3 nM for HGK (MAP4K4) and 23.7 nM for MLK3.
Prostetin/12k rescues cyclopiazonic acid (CPA)-induced neurodegeneration with EC50 of 0.1 uM in motor neuron survival assay.
Prostetin/12k has IC50 of 0.3 nM for HGK in cell-free radiolabeled ATP assays.
Prostetin/12k inhibits MLK3 with IC50 of 23.7 nM, potently inhibits MAP4Ks MINK1, KHS, HGK, GLK, and GCK.
Prostetin/12k significantly and dose-dependently decreased TNFα secretion in LPS-stimulated microglia with EC50 of 0.47 uM.

物理化学性质&存储条件

分子量 446.98
分子式 C26H27ClN4O
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

2-(4-(4-(3-(3-chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)benzyl)piperazin-1-yl)ethan-1-ol

参考文献

1. Bos PH, et al. Cell Chem Biol. 2019 Dec 19;26(12):1703-1715.e37.

2. Moreno R, et al. Eur J Med Chem. 2023 Sep 5;257:115511.

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