ZINC02092166

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ZINC02092166 是一种新型有效、选择性小分子抑制剂，可抑制 β-catenin/Tcf4 蛋白-蛋白相互作用，在 AlphaScreen 和 FP 测定中 Ki 分别为 1.7 和 7.0 uM。

ZINC02092166 is a novel potent, and selective small-molecule inhibitor for the β-catenin/Tcf4 protein-protein interaction with Ki of 1.7 and 7.0 uM in AlphaScreen and FP assay (wild-type β-catenin), respectively; remain affinity for muant catenin V511S, V511S/I569S and R469A with Ki of 20-50 uM; exhibits dual selectivity for β-catenin/Tcf over β-catenin/cadherin and β-catenin/APC PPIs.

LQZ-7F could be hudrolyzed under acidic conditions.LQZ-7F (2.5 μM, 72 hours) displays cytotoxicity towards human cancer cells (PC-3, C4-2) with the IC50s of 2.99 μM and 2.74 μM, respectively.LQZ-7F effectively inhibits survival of all cancer cell lines with IC50 values ranging between 0.4 and 4.4 mM.LQZ-7F (2 μM, 24 hours) disrupts microtubule structure and cause mitotic arrest in P3 cells. Apoptosis Analysis Cell Line:PC3, HL-60 cellsConcentration:0, 5, 10 μM Incubation Time:Result:Caused 54% to 69% apoptosis for PC3 and 66% to 98% apoptosis for HL-60 cells.Cell Cytotoxicity AssayCell Line:PC-3, DU145 Concentration:10, 20 μM Incubation Time:72 hours Result:Showed that the IC50 in human PC3 and DU145 cells was approximately 25 μM.

LQZ-7F (i.p. injection; 25 mg/kg once every 3 days; 24 days) inhibits growth of xenograft tumor and may be due to its induction of surviving degradation in vivo. Animal Model:4- to 6-week-old male NSG (NOD/SCID/IL-2Rg null) mice.Dosage:25 mg/kg Administration:24 days Result:Inhibited growth of xenograft tumors by inhibiting surviving.

ZINC 02092166

Wnt/Notch/Hedgehog

Beta-catenin

Beta-catenin

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354543-09-2

349.27

C14H7N9O3

>98% (HPLC)

——

C1=CC=C2C(=C1)C(=C3C2=NC4=NONC4=N3)N=NC(=O)C5=NON=C5N

(Z)-4-amino-N'-(9H-indeno[1,2-b][1,2,5]oxadiazolo[3,4-e]pyrazin-9-ylidene)-1,2,5-oxadiazole-3-carbohydrazide

(-20℃)

With Ice Pack

≥ 2 years