产品名称

英文名称：PFK15

同义词

PFK-015、4382-63-2、PFK15、1-(Pyridin-4-yl)-3-(quinolin-2-yl)prop-2-en-1-one、(E)-1-pyridin-4-yl-3-quinolin-2-ylprop-2-en-1-one、PFK015、(E)-1-(Pyridin-4-yl)-3-(quinolin-2-yl)prop-2-en-1-one、CHEMBL3105836、2314451-67-5、1-(4-Pyridinyl)-3-(2-quinolinyl)-2-propen-1、(E)-1-(吡啶-4-基)-3-(喹啉-2-基)丙-2-烯-1-酮

产品性质

CAS编号：4382-63-2

分子式：C17H12N2O

分子量：260.29

EC号：809-326-5

PubChem编号：25142799

别名：(E)-1-(吡啶-4-基)-3-(喹啉-2-基)丙-2-烯-1-酮

英文别名：PFK-015|4382-63-2|PFK15|1-(Pyridin-4-yl)-3-(quinolin-2-yl)prop-2-en-1-one|(E)-1-pyridin-4-yl-3-quinolin-2-ylprop-2-en-1-one|PFK015|(E)-1-(Pyridin-4-yl)-3-(quinolin-2-yl)prop-2-en-1-one|CHEMBL3105836|2314451-67-5|1-(4-Pyridinyl)-3-(2-quinolinyl)-2-propen-1

规格或纯度：98% (HPLC)

英文名称：PFK15

生化机理：有力和选择性的6-磷酸果糖-2-激酶（PFK）抑制剂（IC 50 = 207 nM）。在转化细胞中迅速诱导细胞凋亡。抑制癌细胞中葡萄糖的摄取和生长。在体内显示抗肿瘤作用。

储存温度：-20°C储存

运输条件：超低温冰袋运输

备注：如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。

产品介绍：PFK-015是PFKFB3抑制剂，对重组PFKFB3的IC50为110 nM，能抑制肿瘤细胞内PFKFB3活性，IC50为20 nM。PFK-015 is an effective inhibitor of PFKFB3 with IC50 of 110 nM (recombinant PFKFB3) and inhibits PFKFB3 activity in cancer cells with IC50 of 20 nM. IC50 value 110 nM (recombinant PFKFB3)[1] Target PFKFB3 PFK-015 possesses compelling in vitro properties, has satisfactory PK properties in rodents, and suppresses tumor glucose metabolism and growth in an aggressive mouse model of non-small cell lung cancer. PFK-015 is not a Pgp substrate as determined by transport and cell permeability assays in Caco-2 and MDCK-MDR1 (Papp A-B / B-A results 1.8 / 4 and 5 / 5 10–6 cm/s). PFK-015 inhibits cancer cell proliferation in a panel of 17 cancer cell lines. PFK-015 suppresses glucose uptake in cancer cells. Rodent PK studies following IV dosing at 5 mg/kg resulted in a profile with a satisfactory half-life (5.1 hours), exposure (AUCinf 1804 ng.h/ml), tissue distribution (Vd 20.5 L/kg) and reasonable clearance (46.2 mL/min/kg). Also, pre-clinical efficacy studies of C57Bl/6 mice bearing Lewis Lung Carcinoma (LLC) xenografts demonstrated 80% tumor growth inhibition relative to vehicle control. Finally, micro-PET studies performed on mice bearing LLC tumors showed a significant inhibition of tumor 2-[18F]-fluoro-2-deoxy-glucose uptake. These results support further development of PFK-015 as a novel anti-cancer agent.

IUPAC Name：(E)-1-pyridin-4-yl-3-quinolin-2-ylprop-2-en-1-one

INCHI：InChI=1S/C17H12N2O/c20-17(14-9-11-18-12-10-14)8-7-15-6-5-13-3-1-2-4-16(13)19-15/h1-12H/b8-7+

InChi Key：UJJUKZPBUMCSJZ-BQYQJAHWSA-N

Canonical SMILES：C1=CC=C2C(=C1)C=CC(=N2)C=CC(=O)C3=CC=NC=C3

Isomeric SMILES：C1=CC=C2C(=C1)C=CC(=N2)/C=C/C(=O)C3=CC=NC=C3

WGK Germany：3

关联CAS：4382-63-2

PubChem CID：25142799

MeSH Entry Terms：1-(4-pyridinyl)-3-(2-quinolinyl)-2-propen-1-one;PFK15

象形图：

信号词：Warning

危险声明：H315 Causes skin irritationH319 Causes serious eye irritationH335 May cause respiratory irritation

预防措施声明：P261,P305+P351+P338,P280,P302+P352,P321,P405,P501,P264,P271,P304+P340,P403+P233,P362+P364,P264+P265,P337+P317,P332+P317,P319

产品包装