| 公司名称： |
上海波以尔化工有限公司 |
| 联系电话： |
|
| 产品介绍： |
英文名称：FRAX597
CAS：1286739-19-2
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| 公司名称： |
BOC Sciences |
| 联系电话： |
16314854226 |
| 产品介绍： |
英文名称：FRAX597
CAS：1286739-19-2
纯度：>98% 备注：FRAX597 is a potent, ATP-competitive inhibitor of group I PAKs with IC50 of 8 nM, 13 nM, and 19 nM for PAK1, PAK2, and PAK3, respectively. |
| 公司名称： |
上海皓元医药股份有限公司 |
| 联系电话： |
86-21-58998985 |
| 产品介绍： |
英文名称：FRAX597
CAS：1286739-19-2
纯度：>98% 包装信息：1066RMB/2mg 备注：试剂级 |
| 公司名称： |
上海石鑫医药科技有限公司 |
| 联系电话： |
18621020637 |
| 产品介绍： |
英文名称：FRAX597
CAS：1286739-19-2
纯度：98 包装信息：1g/;5g/ |
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| 中文名称: | FRAX597 | | 中文同义词: | 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;化合物FRAX597 | | 英文名称: | 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 | | 英文同义词: | 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;FRAX597;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-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;FRAX597, >=98%;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;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 | | CAS号: | 1286739-19-2 | | 分子式: | C29H28ClN7OS | | 分子量: | 558.1 | | EINECS号: | | | 相关类别: | 小分子抑制剂，天然产物;抑制剂;细胞生物学试剂;Inhibitors;API | | Mol文件: | 1286739-19-2.mol |  |
| 熔点 | >220°C (dec.) | | 储存条件 | Refrigerator | | 溶解度 | DMSO (Slightly) | | 形态 | Solid | | 颜色 | Yellow |
| 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 |
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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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