PF-3758309|898044-15-0|(PF-03758309)-陌孚医药/Medlife

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PF-3758309 (Synonyms: PF-03758309)

目录号: PL08767 纯度: ≥99%

CAS No. :898044-15-0

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中文名称	PF-3758309
中文别名	PF-3758309 抑制剂;(S)-N-(2-(二甲基氨基)-1-苯基乙基)-6,6-二甲基-3-((2-甲基噻吩[3,2-d]嘧啶-4-基)氨基)-4,6-二氢吡咯[3,4-c]吡唑-5(1H)-甲酰胺
英文名称	PF-3758309
英文别名	PF-3758309;N-[(1S)-2-(dimethylamino)-1-phenylethyl]-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl)amino]-1,4-dihydropyrrolo[3,4-c]pyrazole-5-carboxamide;PF 3758309;PK459EA5I2;(S)-N-(2-(dimethylamino)-1-phenylethyl)-6,6-dimethyl-3-((2-methylthieno[3,2-d]pyrimidin-4-yl)amino)-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide;N-((1S)-2-(Dimethylamino)-1-phenylethyl)-6,6-dimethyl-3-((2-methylthieno(3,2-d)pyrimidin-4-yl)amino)-4,6-dihydropyrrolo(3,4;PF-03758309;N-[(1S)-2-(Dimethylamino)-1-phenylethyl]-4,6-dihydro-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl)amino]pyrrolo[3,4-c]pyrazole-5(1H)-carboxamide (ACI);N-[(1S)-2-(Dimethylamino)-1-phenylethyl]-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl)amino]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide;PF 03758309
Cas No.	898044-15-0
分子式	C₂₅H₃₀N₈Os
分子量	490.62
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

PF-3758309 (PF-03758309) 是一种有效的、口服的、可逆的 ATP 竞争性 PAK4 抑制剂 (K_d= 2.7 nM; K_i=18.7 nM)。PF-3758309 具有 PAK4 抑制剂的预期细胞功能：抑制锚定独立生长、诱导凋亡、细胞骨架重塑和抑制增殖。

生物活性

PF-3758309 (PF-03758309) is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (K d = 2.7 nM; K i =18.7 nM). PF-3758309 has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.

性状

Solid

IC50 & Target[1][2]

PAK4 18.7 nM (Ki) PAK1 13.7 nM (Ki)

体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Murray, Brion W., et al. Small-molecule p21-activated kinase inhibitor PF3758309 is a potent inhibitor of oncogenic signaling and tumor growth. Proceedings of the National Academy of Sciences of the United States of America (2010), 107(20), 9446-9451, S94
[2]. Zhao ZS, et al. Do PAKs make good drug targets? F1000 Biol Rep. 2010 Sep 23;2:70.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (203.82 mM)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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