
PF-3758309 hydrochloride
CAS No. 1279034-84-2
PF-3758309 hydrochloride ( —— )
产品货号. M17237 CAS No. 1279034-84-2
PF-3758309,也称为 PF-03758309,是一种 PAK4 抑制剂,也是一种口服生物可利用的 p21 激活激酶 4 (PAK4) 小分子抑制剂,具有潜在的抗肿瘤活性。
纯度: >98% (HPLC)






规格 | 价格/人民币 | 库存 | 数量 |
2MG | ¥405 | 有现货 |
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5MG | ¥599 | 有现货 |
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10MG | ¥972 | 有现货 |
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25MG | ¥1547 | 有现货 |
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50MG | ¥2851 | 有现货 |
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100MG | ¥4479 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称PF-3758309 hydrochloride
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注意事项本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
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产品简述PF-3758309,也称为 PF-03758309,是一种 PAK4 抑制剂,也是一种口服生物可利用的 p21 激活激酶 4 (PAK4) 小分子抑制剂,具有潜在的抗肿瘤活性。
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产品描述PF-3758309, also known as PF-03758309, is a PAK4 inhibitor, is also a n orally bioavailable small-molecule inhibitor of p21-activated kinase 4 (PAK4) with potential antineoplastic activity. PAK4 inhibitor PF-03758309 binds to PAK4, inhibiting PAK4 activity and cancer cell growth. PAK4, a serine/threonine kinase belonging to the p21-activated kinase (PAK) family, is often upregulated in a variety of cancer cell types and plays an important role in cancer cell motility, proliferation, and survival.(In Vitro):PF-3758309 has similar enzymatic potency against the kinase domains of the other group B PAKs (PAK5, Ki=18.1 nM; PAK6, Ki=17.1 nM) and group A PAK1 (Ki=13.7 nM), but is less active against the other two group A PAKs (PAK2, IC50=190 nM; PAK3, IC50=99 nM).In cells, PF-3758309 inhibits phosphorylation of the PAK4 substrate GEF-H1 (IC50=1.3 nM) and anchorage-independent growth of a panel of tumor cell lines (IC50=4.7 nM).PF-3758309 also inhibits endogenous pGEF-H1 accumulation in HCT116 cells. PF-3758309 potently inhibits cellular proliferation (IC50=20 nM) and anchorage-independent growth (IC50=27 nM) of A549 cells.(In Vivo):PF-3758309 (7.5-30 mg/kg; p.o.; twice daily for 9-18 days) results in statistically significant tumor growth inhibition (TGI) in HCT116 and A549 models.
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体外实验PF-3758309 hydrochloride has similar enzymatic potency against the kinase domains of the other group B PAKs (PAK5, Ki=18.1 nM; PAK6, Ki=17.1 nM) and group A PAK1 (Ki=13.7 nM), but is less active against the other two group A PAKs (PAK2, IC50=190 nM; PAK3, IC50=99 nM). In cells, PF-3758309 hydrochloride inhibits phosphorylation of the PAK4 substrate GEF-H1 (IC50=1.3 nM) and anchorage-independent growth of a panel of tumor cell lines (IC50=4.7 nM). PF-3758309 hydrochloride also inhibits endogenous pGEF-H1 accumulation in HCT116 cells. PF-3758309 potently inhibits cellular proliferation (IC50=20 nM) and anchorage-independent growth (IC50=27 nM) of A549 cells.
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体内实验PF-3758309 hydrochloride (7.5-30 mg/kg; p.o.; twice daily for 9-18 days) results in statistically significant tumor growth inhibition (TGI) in HCT116 and A549 models. Animal Model:Female nu/nu, CRL breed 6–8 weeks old mice (bearing HCT116 and A549 tumors) Dosage:7.5-30 mg/kg Administration:Oral administration; twice daily for 9-18 days Result:Significant tumor growth inhibition (TGI) in HCT116 and A549 models.
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同义词——
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通路Others
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靶点Other Targets
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受体PAK4| PAK1| PAK6| PAK5| PAK3
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研究领域——
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适应症——
化学信息
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CAS Number1279034-84-2
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分子量527.08
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分子式C25H31ClN8OS
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纯度>98% (HPLC)
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溶解度——
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SMILESCl.CN(C)C[C@@H](NC(=O)N1Cc2c(n[nH]c2Nc2nc(C)nc3ccsc23)C1(C)C)c1ccccc1
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Briz V, Baudry M.2014 Feb 25;5:22. doi: 10.3389/fendo.2014.00022. eCollection 2014. PubMed PMID: 24611062; PubMed Central PMCID: PMC3933789.
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