660868-91-7

中文名稱 3-[2-(三氟甲基)芐氧基]-5-(5,6-二甲氧基-1H-苯并[D]咪唑-1-基)-2-噻吩甲酰胺

英文名稱 GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide

CAS 660868-91-7

分子式 C22H18F3N3O4S

分子量 477.46

MOL 文件 660868-91-7.mol

更新日期 2026/06/01 11:31:36

660868-91-7 結(jié)構(gòu)式

基本信息物理化學性質(zhì) 安全數(shù)據(jù) 圖譜信息 3-[2-(三氟甲基)芐氧基]-5-(5,6-二甲氧基-1H-苯并[D]咪唑-1-基)-2-噻吩甲酰胺價格(試劑級) 常見問題列表

基本信息

中文別名

PLK1和PLK3抑制劑(GW843682X)
3-[2-(三氟甲基)芐氧基]-5-(5,6-二甲氧基-1H-苯并[D]咪唑-1-基)-2-噻吩甲酰胺

英文別名

GW843682
GW843682X
Polo-like Kinase Inhibitor III
GW843682X
GW 843682X
GW843682
GW-843682X
Polo-like Kinase Inhibitor III - CAS 660868-91-7 - Calbiochem
2-Thiophenecarboxamide, 5-(5,6-dimethoxy-1H-benzimidazol-1-yl)-3
5-(5,6-dimethoxy-1-benzimidazolyl)-3-[[2-(trifluoromethyl)phenyl]methoxy]-2-thiophenecarboxamide
5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide
3-(2-(Trifluoromethyl)benzyloxy)-5-(5,6-dimethoxy-1H-benzo[d]imidazol-1-yl)thiophene-2-carboxamide
5-(5,6-dimethoxy-1H-benzo[d]imidazol-1-yl)-3-((2-(trifluoromethyl)benzyl)oxy)thiophene-2-carboxamide

所屬類別

生物化工：激動劑抑制劑

物理化學性質(zhì)

沸點609.1±65.0 °C(Predicted)

密度1.45±0.1 g/cm3(Predicted)

儲存條件2-8°C

溶解度二甲基亞砜：>10mg/mL

酸度系數(shù)(pKa)15.03±0.50(Predicted)

形態(tài)固體

顏色米白色

InChI1S/C22H18F3N3O4S/c1-30-16-7-14-15(8-17(16)31-2)28(11-27-14)19-9-18(20(33-19)21(26)29)32-10-12-5-3-4-6-13(12)22(23,24)25/h3-9,11H,10H2,1-2H3,(H2,26,29)

InChIKeyJSKUWFIZUALZLX-UHFFFAOYSA-N

SMILESCOc1cc2ncn(-c3cc(OCc4ccccc4C(F)(F)F)c(s3)C(N)=O)c2cc1OC

安全數(shù)據(jù)

危險性符號(GHS) 有害 (GHS07)

GHS07

警示詞警告

危險性描述H315-H319-H335-H413

防范說明P261-P305+P351+P338

危險品標志Xi

危險類別碼36/37/38

安全說明26-36/37

WGK Germany3

存儲類別11 - Combustible Solids

圖譜信息

3-[2-(三氟甲基)芐氧基]-5-(5,6-二甲氧基-1H-苯并[D]咪唑-1-基)-2-噻吩甲酰胺(660868-91-7)核磁圖(¹HNMR)

3-[2-(三氟甲基)芐氧基]-5-(5,6-二甲氧基-1H-苯并[D]咪唑-1-基)-2-噻吩甲酰胺價格(試劑級)

報價日期	產(chǎn)品編號	產(chǎn)品名稱	CAS號	包裝	價格
2025/12/22	HY-11003	3-[2-(三氟甲基)芐氧基]-5-(5,6-二甲氧基-1H-苯并[D]咪唑-1-基)-2-噻吩甲酰胺 GW843682X	660868-91-7	1 mg	310元
2025/12/22	HY-11003	3-[2-(三氟甲基)芐氧基]-5-(5,6-二甲氧基-1H-苯并[D]咪唑-1-基)-2-噻吩甲酰胺 GW843682X	660868-91-7	5mg	700元
2025/12/22	HY-11003	3-[2-(三氟甲基)芐氧基]-5-(5,6-二甲氧基-1H-苯并[D]咪唑-1-基)-2-噻吩甲酰胺 GW843682X	660868-91-7	10mM * 1mLin DMSO	735元

常見問題列表

生物活性

GW843682X 是一種選擇性的，ATP-競爭性的 PLK1 and PLK3 抑制劑，IC50 值分別為 2.2 nM and 9.1 nM，選擇性是其他 30 種激酶的 100 多倍。

靶點

PLK1

2.2 nM (IC ₅₀ )

PLK3

9.1 nM (IC ₅₀ )

PDGFR1β

160 nM (IC ₅₀ )

VEGFR2

360 nM (IC ₅₀ )

Aurora A

4800 nM (IC ₅₀ )

CDK2/cyclin A

7600 nM (IC ₅₀ )

體外研究

GW843682X (compound 1) is effective on inhibition of growth of tumor cells, with IC ₅₀ s of 0.41, 0.57, 0.11, 0.38, and 0.70 μM for A549, BT474, HeLa, H460 and HCT116 cell lines. GW843682X dose-dependently inhibits PLK1 phosphorylation of Ser15-p53, with an IC ₅₀ of 0.14 μM. GW843682X (3 μM) causes a strong G2-M arres in HDF cells and H460 cells after treatment for 24, 48, and 72 h. GW843682X (5 μM) leads to apoptosis in H460 cells instead of HDF cells. GW843682X inhibits proliferation of U937 cells with an EC ₅₀ of 120 nM. GW843682X (500 nM) in combination with 5 μM VP-16 suppresses 50% of entry into mitosis in U937 cells. GW843682X (0.06-1?μM) has inhibitory activities against proliferation of acute leukemia cells, and potentiates the anti-proliferative activity of vincristine. Moreover, GW843682X (0.1-1?μM) induces apoptosis of leukemia cells in a dose- and time-dependent manner. GW843682X (0.5-1?μM) dephosphorylates Bcl-xl in leukemia cells.