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PF-3758309

PF-3758309

品 牌 MCE
C A S 号 898044-15-0
货 号 HY-13007
规 格 5mg
价 格(元) 550.00
咨询优惠价
货号 规格 价格
HY-13007 5mg 550.00
HY-13007 10mg 800.00
HY-13007 50mg 2600.00
HY-13007 100mg 4400.00

产品说明


PF-3758309是PAK4抑制剂,IC50为1.3 nM,能抑制HCT116,A549,M24met和别的肿瘤外植体模型。



PF-3758309的生物活性


PF-3758309 is a inhbitor of PAKs with IC50 of 1.3 nM for PAK4; inhbits tumor growth in HCT116, A549, M24met and other xenograft tumor models..
IC50 Value: 1.3 nM (PAK4)
Target: PAKs
in vitro: PF-3758309, a potent (K(d) = 2.7 nM), ATP-competitive, pyrrolopyrazole inhibitor of PAK4. In cells, PF-3758309 inhibits phosphorylation of the PAK4 substrate GEF-H1 (IC(50) = 1.3 nM) and anchorage-independent growth of a panel of tumor cell lines (IC(50) = 4.7 +/- 3 nM). PF-3758309, which exhibits relatively good selectivity and high potency for PAKs. Experiments using PF-3758309 confirm that inhibiting PAK is a beneficial strategy to combat some tumors, and this activity is likely related to modulation of both cell proliferation and survival.
in vivo: Researcher used a nude mouse xenograft model of 2-S (HCT116 and RKO) and 2-R (SW948 and GEO) CRC cell lines and treated them with PF-3758309 for 14 days. Tumor volumes were measured twice weekly throughout the experiment and the responses of the xenografts were consistent with the in vitro cell line results, i.e., HCT116 and RKO CRC cell lines exhibited a statistically significant tumor growth inhibition (p = 0.009 and 0.03, respectively) compared to vehicle, and responsiveness was associated with greater expression of the mesenchymal-associated genes, vimentin and caldesmon.

化学信息


分子量 490.62 储存条件 参考CoA中推荐的条件进行储存。
分子式 C₂₅H₃₀N₈OS
CAS号 898044-15-0
溶剂/溶解度 10 mM in DMSO

相关文献


[1]. Murray, Brion W.; Guo, Chuangxing; Piraino, Joseph. 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, S9446/1-S9446/18.
[2]. Murray BW, Guo C, Piraino J, Westwick JK, Zhang C, Lamerdin J, Dagostino E, Knighton D, Loi CM, Zager M, Kraynov E, Popoff I, Christensen JG, Martinez R, Kephart SE, Marakovits J, Karlicek S, Bergqvist S, Smeal T. Small-molecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growth. Proc Natl Acad Sci U S A. 2010 May 18;107(20):9446-51.
[3]. Zhao ZS, Manser E. Do PAKs make good drug targets? F1000 Biol Rep. 2010 Sep 23;2:70.