Conteltinib

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

CT-707 (Conteltinib) 是一种针对 FAK 的新型多激酶抑制剂 (IC50=1.6 nM)。

CT-707 (Conteltinib) is a novel multikinase inhibitor targeting FAK (IC50=1.6 nM), ALK and Pyk2, exerts synergistic antitumor effects against hepatocellular carcinoma in vitro and in vivo; effectively inhibits the activation of FAK induced by cabozantinib; displays potent activities in arresting cancer cell growth, promoting cell detachment, and decreasing wound healing, also exhibits potent anticancer activities in vivo, inhibits tumor growth and metastasis in T47D, Karpas299, and 4T1 xenograft models.Lung Cancer Phase 1 Clinical.

Cell Viability Assay Cell Line:The human hepatocellular carcinoma cell lines HepG2 and Bel-7402 Concentration:1.0, 1.5, 2.0, 2.5, and 3.0 μM for HepG2 cells; 0.2, 0.4, 0.8, 1.5, and 3.0 μM for Bel-7402 cells Incubation Time:72 hours Result:When cells were exposed to XL184 (5 μM), Conteltinib (3 μM), or their combination, the survival rates were 57.3%, 39.3%, and 11.2%, respectively, in HepG2; those in Bel-7402 were 57.8%, 61.6%, and 34.2%, respectively.Apoptosis Analysis Cell Line:HepG2 and Bel-7402 cells Concentration:3 μM Incubation Time:48 hours Result:The apoptosis rates of control, XL184, Conteltinib, and combination groups in HepG2 were 5.0%, 10.5%, 18.4%, and 41.1%, respectively, and those in Bel-7402 were 4.4%, 16.3%, 8.7%, and 36.4%, respectively. Western Blot Analysis Cell Line:HepG2 and Bel-7402 Concentration:3 μM Incubation Time:24 hours Result:Could markedly decrease FAK phosphorylation induced by XL184, which might partially account for the synergetic effect.

Animal Model:Nude mice transplanted with HepG2 xenografts Dosage:50 mg/kg Administration:Intragastrically (i.g.) twice a day for first 3 days, 7th, 8th, 11th, 12th, and 14th days; once a day for 4th, 6th, 9th, 10th, and 13th days; no administration for the 5th day.Result:Caused a moderate decrease in the relative tumor volume (RTV).The inhibition rate of combination group reached 77.4%, whereas the mono-treatment of XL184 or CT-707 alone caused 30.7% and 19.4% inhibition in the tumor weight, respectively.

CT-707

Angiogenesis

FAK

FAK

Cancer

Lung Cancer

1384860-29-0

635.832

C32H45N9O3S

>98% (HPLC)

In Vitro:?DMSO : 31.25 mg/mL (49.15 mM)

O=S(C1=CC=CC=C1NC2=C3C(NCC3)=NC(NC4=CC=C(N5CCC(N6CCN(C)CC6)CC5)C=C4OC)=N2)(NC(C)C)=O

2-[(2-{2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]anilino}-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]-N-(propan-2-yl)benzene-1-sulfonamide

(-20℃)

With Ice Pack

≥ 2 years