生物活性 体外研究 体内研究 靶点 FRAX597 试剂级价格
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FRAX597

FRAX597,1286739-19-2,结构式
FRAX597
  • CAS号:1286739-19-2
  • 英文名:6-(2-Chloro-4-thiazol-5-yl-phenyl)-8-ethyl-2-[4-(4-Methyl-piperazin-1-yl)-phenylaMino]-8H-pyrido[2,3-d]pyriMidin-7-one
  • 中文名:FRAX597
  • CBNumber:CB12663792
  • 分子式:C29H28ClN7OS
  • 分子量:558.1
  • MOL File:1286739-19-2.mol
FRAX597化学性质
  • 熔点 :>220°C (dec.)
  • 储存条件 :Refrigerator
  • 溶解度 :DMSO (Slightly)
  • 形态 :Solid
  • 颜色 :Yellow

FRAX597性质、用途与生产工艺

  • 生物活性 FRAX597是一种有效的,ATP竞争性的第一类PAKs抑制剂,对PAK1,PAK2,和 PAK3 的 IC50 分别为 8 nM,13 nM,和 19 nM。
  • 体外研究 FRAX597 (100 n M) displays a significant inhibitory capacity toward YES1 (87%), RET (82%), CSF1R (91%), TEK (87%), PAK1 (82%), and PAK2 (93%), while displays minimal inhibitory activity towards the group II PAKs: PAK4 (0%), PAK6 (23%), and PAK7 (8%). FRAX597 treatment dramatically impairs the proliferation of Nf2-null SC4 Schwann cells (SC4 cells). FRAX597 displays an IC50 value of 48 nM against wild type PAK1, while IC 50 values against the V342F and V342Y PAK1 mutants are higher than 3μM and 2 μM, respectively. FRAX597 inhibits the proliferation and motility of both benign (Ben-Men1, 3μM) and malignant (KT21-MG1, 0.4 μM) meningiomas cells after treating of 72 h.
  • 体内研究 In NOD/SCID mice which bearing Nf2-/-SC4 Schwann cells, FRAX597 (100 mg/kg/day, p.o.) causes more significant tumor growth inhibition cpmpared with control mice. In SCID mice with orthotopic meningioma, FRAX597 (90 mg/kg/day, p.o.) significantly suppresses tumor growth. In KrasG12D mice, treatment with FRAX597 (90 mg/kg/day, p.o.) causes tumor regression and loss of Erk and Akt activity.
  • 靶点

    PAK1

    8 nM (IC 50 )

    PAK2

    13 nM (IC 50 )

    PAK3

    19 nM (IC 50 )

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FRAX597 试剂级价格
  • 更新日期:2024/04/30
  • 产品编号:HY-15542A
  • 产品名称:FRAX597 FRAX597
  • CAS编号:1286739-19-2
  • 包装:2mg
  • 价格:400元
  • 更新日期:2024/04/30
  • 产品编号:HY-15542A
  • 产品名称:FRAX597 FRAX597
  • CAS编号:1286739-19-2
  • 包装:5mg
  • 价格:850元
FRAX597生产厂家
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