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- 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
- 英文别名:
- FRAX597;CS-1774;FRAX597, >=98%;FRAX 597;FRAX-597;FRAX597;FRAX597,FRAX-597,p21 activated kinases,FRAX 597,Inhibitor,inhibit,PAK;6-[2-chloro-4-(1,3-thiazol-5-yl)phenyl]-8-ethyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrido[2,3-d]pyrimidin-7-one;6-(2-chloro-4-(thiazol-5-yl)phenyl)-8-ethyl-2-(4-(4-methylpiperazin-1-yl)phenylamino)pyrido[2,3-d]pyrimidin-7(8H)-one;6-[2-Chloro-4-(5-thiazolyl)phenyl]-8-ethyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one;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;Pyrido[2,3-d]pyriMidin-7(8H)-one, 6-[2-chloro-4-(5-thiazolyl)phenyl]-8-ethyl-2-[[4-(4-Methyl-1-piperazinyl)phenyl]aMino]-
- 中文名:
- FRAX597
- 中文别名:
- 化合物FRAX597;FRAX 597,I类PAK抑制剂;I型P21激活激酶(PAK)抑制剂(FRAX597);6-(2-氯-4-(噻唑-5-基)苯基)-8-乙基-2-((4-(4-甲基哌嗪-1-基)苯基)氨基)吡啶并[2,3-D]嘧啶-7(8H)-酮
- CBNumber:
- CB12663792
- 分子式:
- C29H28ClN7OS
- 分子量:
- 558.1
- MOL File:
- 1286739-19-2.mol
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FRAX597性质、用途与生产工艺
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。
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.
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 Kras
G12D mice, treatment with FRAX597 (90 mg/kg/day, p.o.) causes tumor regression and loss of Erk and Akt activity.
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PAK1
8 nM (IC
50
)
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PAK2
13 nM (IC
50
)
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PAK3
19 nM (IC
50
)
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FRAX597
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