1286739-19-2
中文名稱(chēng)
FRAX597
英文名稱(chēng)
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
CAS
1286739-19-2
分子式
C29H28ClN7OS
分子量
558.097
MOL 文件
1286739-19-2.mol
更新日期
2024/06/07 17:53:10
1286739-19-2 結(jié)構(gòu)式
基本信息
中文別名
化合物FRAX597I型P21激活激酶(PAK)抑制劑(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
英文別名
CS-1774FRAX597
FRAX597, >=98%
FRAX 597
FRAX-597
FRAX597
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]-
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 USP/EP/BP
所屬類(lèi)別
生物化工：PAK 抑制劑
常見(jiàn)問(wèn)題列表
生物活性
FRAX597是一種有效的，ATP競(jìng)爭(zhēng)性的第一類(lèi)PAKs抑制劑，對(duì)PAK1，PAK2，和 PAK3 的 IC50 分別為 8 nM，13 nM，和 19 nM。體外研究
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.體內(nèi)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.靶點(diǎn)
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PAK1 8 nM (IC 50 ) |
PAK2 13 nM (IC 50 ) |
PAK3 19 nM (IC 50 ) |