SML2618
FRAX1036
≥98% (HPLC)
别名:
6-(2-Chloro-4-(6-methylpyrazin-2-yl)phenyl)-8-ethyl-2-((2-(1-methylpiperidin-4-yl)ethyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one, 6-[2-Chloro-4-(6-methyl-2-pyrazinyl)phenyl]-8-ethyl-2-[[2-(1-methyl-4-piperidinyl)ethyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one, FRAX 1036, FRAX-1036
登录查看公司和协议定价
所有图片(1)
About This Item
推荐产品
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
−20°C
SMILES字符串
Clc1c(ccc(c1)c5nc(cnc5)C)c2[c]([n](c3nc(ncc3c2)NCCC4CCN(CC4)C)CC)=O
InChI
1S/C28H32ClN7O/c1-4-36-26-21(16-32-28(34-26)31-10-7-19-8-11-35(3)12-9-19)13-23(27(36)37)22-6-5-20(14-24(22)29)25-17-30-15-18(2)33-25/h5-6,13-17,19H,4,7-12H2,1-3H3,(H,31,32,34)
InChI key
RYCBSFIKWACFBY-UHFFFAOYSA-N
生化/生理作用
FRAX1036 is a potent, group I-selective p21-activated kinase (PAK) inhibitor (PAK1/4 Ki = 23 nM/1.4 μM; PAK1/4 IC50 = 2 nM/>500 nM; >96% PAK1/2/3 inhibition vs. 5.1%/8.2%/22.2% PAK4/5/6 inhibition at 1 μM) with significant inhibitory activity toward only 11 other kinases at a high concentration of 1 μM (78.7-100% inhibition) among a panel of 240. FRAX1036 exhibits higher antiproliferation activity in PAK negative regulator NF2-deficient meningioma cultures (NF2-/- Ben-Men-1/KT21-MG1 IC50 = 1.888/1.991 μM vs.NF2+/+ MN328/MN525 IC50 = 4.239/3.296 μM) by inhibiting cellular PAK autophosphorylation and downstream signaling events. When administered orally in a murine orthotopic meningioma model, FRAX1036 effectively suppresses the growth of established KT21 and Ben-Men tumors in vivo (30 mg/kg/d p.o.).
Orally active, potent group I-selective p21-activated kinase (PAK1/2/3) inhibitor with in vivo efficacy in a murine orthotopic meningioma model.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
G Semenova et al.
Oncogene, 36(38), 5421-5431 (2017-05-24)
Malignant peripheral nerve sheath tumors (MPNSTs) are devastating sarcomas for which no effective medical therapies are available. Over 50% of MPSNTs are associated with mutations in NF1 tumor suppressor gene, resulting in activation of Ras and its effectors, including the
p21-Activated Kinase 2 Regulates Endothelial Development and Function through the Bmk1/Erk5 Pathway.
Maria Radu et al.
Molecular and cellular biology, 35(23), 3990-4005 (2015-09-24)
p21-activated kinases (Paks) have been shown to regulate cytoskeleton rearrangements, cell proliferation, attachment, and migration in a variety of cellular contexts, including endothelial cells. However, the role of endothelial Pak in embryo development has not been reported, and currently, there
Tatiana Y Prudnikova et al.
Small GTPases, 8(4), 193-198 (2016-07-19)
The p21-activated kinases (PAKs) are Cdc42/Rac-activated serine-threonine protein kinases that regulate several key cancer-relevant signaling pathways, such as the Mek/Erk, PI3K/Akt, and Wnt/β-catenin cascades. Pak1 is frequently overexpressed and/or hyperactivated in different human cancers, including breast, ovary, prostate, and brain
Joachim Rudolph et al.
Journal of medicinal chemistry, 58(1), 111-129 (2014-11-22)
The p21-activated kinase (PAK) family of serine/threonine protein kinases plays important roles in cytoskeletal organization, cellular morphogenesis, and survival, and members of this family have been implicated in many diseases including cancer, infectious diseases, and neurological disorders. Owing to their
T Y Prudnikova et al.
Oncogene, 35(17), 2178-2185 (2015-08-11)
p21-activated kinases (Paks) are Cdc42/Rac-activated serine-threonine protein kinases that regulate several key cancer-relevant signaling pathways, such as the Mek/Erk, PI3K/Akt and Wnt/b-catenin signaling pathways. Pak1 is frequently overexpressed and/or hyperactivated in different human cancers, including human breast, ovary, prostate and
我们的科学家团队拥有各种研究领域经验，包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.
联系技术服务部门