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PF-3758309 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PF-3758309 hydrochloride图片
CAS NO:1279034-84-2
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
PF-03758309 hydrochloride
产品介绍
PF-3758309 (PF-03758309) hydrochloride 是一种有效的、口服的、可逆的 ATP 竞争性PAK4抑制剂 (Kd= 2.7 nM;Ki=18.7 nM)。PF-3758309 hydrochloride 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) hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor ofPAK4(Kd= 2.7 nM;Ki=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of aPAK4inhibitor: inhibition of anchorage-independent growth, induction ofapoptosis, cytoskeletal remodeling, and inhibition of proliferation[1][2][3].

IC50& Target[1]

PAK4

18.7 nM (Ki)

PAK1

13.7 nM (Ki)

PAK5

18.1 nM (Ki)

PAK6

17.1 nM (Ki)

PAK2

190 nM (IC50)

PAK3

99 nM (IC50)

PAK4

2.7 nM (Kd)

体外研究
(In Vitro)

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)[1].
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)[1].
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[1].

体内研究
(In Vivo)

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[1].

Animal Model:Female nu/nu, CRL breed 6–8 weeks old mice (bearing HCT116 and A549 tumors)[1]
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.
Clinical Trial
分子量

527.08

Formula

C25H31ClN8OS

CAS 号

1279034-84-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.