1380672-07-0
1380672-07-0 結(jié)構(gòu)式
基本信息
TANKYRASE抑制劑(G007-LK)
4-[5-[(1E)-2-[4-(2-氯苯基)-5-[5-(甲基磺?；?-2-吡啶基]-4H-1,2,4-三唑-3-基]乙烯基]-1,3,4-惡二唑-2-基]苯甲腈
CS-1659
G007 LK
G007LK
G007-LK
G007 LK
G007LK
Tankyrase 1/2 Inhibitor VI, G007-LK - Calbiochem
(E)-4-(5-(2-(4-(2-chlorophenyl)-5-(5-(methylsulfonyl)pyridin-2-yl)-4H-1,2,4-triazol-3-yl)vinyl)-1,3,4-oxadiazol-2-yl)benzonitrile
4-[5-[(1E)-2-[4-(2-Chlorophenyl)-5-[5-(methylsulfonyl)-2-pyridinyl]-4H-1,2,4-triazol-3-yl]ethenyl]-1,3,4-oxadiazol-2-yl]benzonitrile
Benzonitrile, 4-[5-[(1E)-2-[4-(2-chlorophenyl)-5-[5-(methylsulfonyl)-2-pyridinyl]-4H-1,2,4-triazol-3-yl]ethenyl]-1,3,4-oxadiazol-2-yl]-
物理化學(xué)性質(zhì)
| 報(bào)價(jià)日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
| 2024/11/08 | HY-12438 | G007-LK G007-LK | 1380672-07-0 | 2mg | 800元 |
| 2024/11/08 | S7239 | G007-LK G007-LK | 1380672-07-0 | 5mg | 1188.88元 |
| 2024/11/08 | HY-12438 | G007-LK G007-LK | 1380672-07-0 | 5mg | 1200元 |
常見問題列表
| Target | Value |
|
TNKS2
(Cell-free assay) | 25 nM |
|
TNKS1
(Cell-free assay) | 46 nM |
G007-LK is a potent inhibitor of TNKS1 and TNKS2, with IC 50 s of 46 nM and 25 nM, respectively, and a cellular IC 50 of 50 nM. G007-LK shows no inhibition of PARP1 at doses up to 20 μM, and has a high CYP3A4 inhibition IC 50 value (>25 μM). G007-LK (0-20 μM) dose-dependently inhibits hepatocellular carcinoma (HCC) cell growth. G007-LK also downregulates the levels of YAP by upregulating AMOTL1 and AMOTL2 in HCC cell lines. In addition, G007-LK (0-20 μM) synergizes with MEK and AKT inhibitors to suppress HCC cell proliferation.
G007-LK displays great pharmacokinetic profile in ICR mice. G007-LK (100 mg/kg chow, p.o.) significantly reduces lineage tracing from LGR5 + intestinal stem cells in mice. G007-LK (100 mg/kg chow, p.o.) specifically targets LGR5 + WNT-dependent intestinal stem cells in Lgr5-EGFP-CreERT2;R26R-tdTomato mice. G007-LK (10, 50 mg/kg, p.o.) also suppressses canonical WNT signalling. Furthermore, G007-LK (100, 1000 mg/kg chow, p.o) shows no effect on the alteration of duodenal morphology.