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
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关于此项目
经验公式（希尔记法）:
C28H32ClN7O
化学文摘社编号:
分子量:
518.05
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
SMILES string
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
Biochem/physiol Actions
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable