产品名称

英文名称：PF-3758309

同义词

PF-3758309、898044-15-0、PF-03758309、(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、PF3758309、PK459EA5I2、N-((1S)-2-(Dimethylamino)-1-phenylethyl)-6,6-di

产品性质

CAS编号：898044-15-0

分子式：C25H30N8OS

分子量：490.62

EC号：804-641-4

PubChem编号：25227462

英文别名：PF-3758309|898044-15-0|PF-03758309|(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|PF3758309|PK459EA5I2|N-((1S)-2-(Dimethylamino)-1-phenylethyl)-6,6-di

规格或纯度：98%

英文名称：PF-3758309

生化机理：PF-3758309 is an orally bioavailable small-molecule inhibitor of p21-activated kinase 4 (PAK4) with potential antineoplastic activity. PAK4 inhibitor PF-3758309 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.

储存温度：-20°C储存

运输条件：超低温冰袋运输

产品介绍：产品介绍PF-03758309是PAK4的抑制剂，其IC50值为1.3 nM。p21活化激酶（PAKs）属于丝氨酸/苏氨酸激酶家族，通过Rho GTP酶调节细胞骨架重组以及核信号。PAK4属于PAKs家族，特异性地与Cdc42-GTP和JNK-GTP相互作用。PAK4参与丝状伪足形成，在肌动蛋白细胞骨架重组中起着重要作用。生化研究表明，PF-3758309是ATP竞争性的PAK4抑制剂，可以抑制激酶活性。使用各种肿瘤细胞系筛选PAK4，PF-3758309抑制PAK4底物（GEF-H1）磷酸化和PAK4诱导的锚定非依赖性细胞生长，其IC50值分别为1.3 nM和4.7 ±3 nM。使用各种PAKs相关激酶筛选PF-3758309，PF-3758309对PAK4显示出良好效应及选择性。细胞分析表明，PF-3758309可以调节PAK4依赖性信号节点，并与p53信号通路相关。PF-03758309 (PF-03758309) 是一种ATP竞争性的p21-activated kinase (PAK)抑制剂，其作用于PAK4的IC50为1.3 nM。PF-3758309 具有抗增殖的作用，在HCT116肿瘤模型中可诱导凋亡。

ALogP：3.1

PubChem SID：488200784

PubChem SID url：https//pubchem.ncbi.nlm.nih.gov/substance/488200784

IUPAC Name：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

INCHI：InChI=1S/C25H30N8OS/c1-15-26-18-11-12-35-20(18)23(27-15)29-22-17-13-33(25(2,3)21(17)30-31-22)24(34)28-19(14-32(4)5)16-9-7-6-8-10-16/h6-12,19H,13-14H2,1-5H3,(H,28,34)(H2,26,27,29,30,31)/t19-/m1/s1

InChi Key：AYCPARAPKDAOEN-LJQANCHMSA-N

Canonical SMILES：CC1=NC2=C(C(=N1)NC3=NNC4=C3CN(C4(C)C)C(=O)NC(CN(C)C)C5=CC=CC=C5)SC=C2

Isomeric SMILES：CC1=NC2=C(C(=N1)NC3=NNC4=C3CN(C4(C)C)C(=O)N[C@H](CN(C)C)C5=CC=CC=C5)SC=C2

关联CAS：898044-15-0

PubChem CID：25227462

MeSH Entry Terms：PF 3758309;PF-3758309;PF3758309

溶解性：≥24.53 mg/mL in DMSO; insoluble in H2O; ≥101.4 mg/mL in EtOH with gentle warming and ultrasonic

象形图：

信号词：Danger

危险声明：H301 Toxic if swallowed

预防措施声明：P321,P405,P501,P264,P270,P330,P301+P316

产品包装