计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Conteltinib (CT-707) is a multi-kinase inhibitor targeting FAK , ALK, and Pyk2 . Conteltinib exerts significant inhibitory effect on FAK with an IC 50 of 1.6 nM
In Vitro
Conteltinib (CT-707) synergizes with XL184 to suppress hepatocellular carcinoma by blocking XL184-induced FAK activation. ?\nThe combination of XL184 (5 μM) and Conteltinib (3 μM) significantly reduces the survival fraction, compared with each agent alone. ?\nThe combination of XL184 (5 μM) and Conteltinib (3 μM) results in enhanced caspase-dependent apoptosis in human hepatocellular carcinoma cell lines. ?\nThe FAK phosphorylation induced by XL184 (5 μM) might be involved in the synergistic antitumor effect of Conteltinib (3 μM) and XL184. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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 AnalysisCell 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 AnalysisCell 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.
In Vivo
The combination of XL184? (20 mg/kg once daily for first 3 days; i.g. 10 mg/kg once a day for 4th day; no administration from 5th to 10th days; i.g. 10 mg/kg once a day from the 10th to 14th days )and CT-707? (i.g. 50 mg/kg 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) shows? the synergistic antitumor effect in HepG2 xenograft nude mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.
IC50& Target:IC50: 1.6 nM (FAK)
规格
别名
康泰替尼
规格或纯度
10mM in DMSO
英文名称
Conteltinib
生化机理
康替替尼（Conteltinib，CT-707）是一种针对FAK、ALK和Pyk2的多激酶抑制剂。Conteltinib 对 FAK 有明显的抑制作用，IC 50 为 1.6 nM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CC(C)NS(=O)(=O)C1=CC=CC=C1NC2=NC(=NC3=C2CCN3)NC4=C(C=C(C=C4)N5CCC(CC5)N6CCN(CC6)C)OC
关联CAS
PubChem CID
MeSH Entry Terms
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;conteltinib;CT-707
分子量
635.82
技术文档
高级数据
产品属性
| ALogP | 5.1 |
|---|
关联靶点（人）
PTK2
Tclin
粘着斑激酶1(Focal adhesion kinase 1)
(0 活性数据)
PTK2B
Tclin
蛋白酪氨酸激酶 2-β(Protein-tyrosine kinase 2-beta)
(0 活性数据)
安全和危险性（GHS）
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品应如何储存？
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 1384860-29-0，分子式为 C32H45N9O3S，分子量为 635.82 g/mol。
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